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TW520274B - Fungicidal mixtures based on tris (oxime ether) derivatives and insecticides - Google Patents

Fungicidal mixtures based on tris (oxime ether) derivatives and insecticides Download PDF

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Publication number
TW520274B
TW520274B TW088104751A TW88104751A TW520274B TW 520274 B TW520274 B TW 520274B TW 088104751 A TW088104751 A TW 088104751A TW 88104751 A TW88104751 A TW 88104751A TW 520274 B TW520274 B TW 520274B
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Taiwan
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compound
patent application
alkyl
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methyl
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TW088104751A
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Chinese (zh)
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Klaus Schelberger
Thomas Grote
Hubert Sauter
Eberhard Ammermann
Gisela Lorenz
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Basf Ag
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    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N37/00Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
    • A01N37/44Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a nitrogen atom attached to the same carbon skeleton by a single or double bond, this nitrogen atom not being a member of a derivative or of a thio analogue of a carboxylic group, e.g. amino-carboxylic acids
    • A01N37/50Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a nitrogen atom attached to the same carbon skeleton by a single or double bond, this nitrogen atom not being a member of a derivative or of a thio analogue of a carboxylic group, e.g. amino-carboxylic acids the nitrogen atom being doubly bound to the carbon skeleton

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  • Life Sciences & Earth Sciences (AREA)
  • Agronomy & Crop Science (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Dentistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Environmental Sciences (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

Mixtures for crop protection, comprising as active components (a) phenylacetic acid derivatives of formula I in which the substituents and the index are each as defined in the description, and their salts, and (b) at least one compound of the formulae II, V, X and XI in a synergistically effective amount. A mixture for crop protection, comprising as active components (a) phenylacetic acid derivatives of the formula (I) in which the substituents and the index have the following meaning: X is NOCH3; Y is NR; R1, R independently of one another are each hydrogen or C1-C4-alkyl; R3 is hydrogen or C1-C4-alkyl; R4, R6 independently of one another are each hydrogen or C1-C4-alkyl; R5 is hydrogen or C1-C4-alkyl; and their salts, and (b) at least one compound of formulae (II), (V), (X) and (XI) in a synergistically effective amount.

Description

〜υζ/4 、發明說明(1 ) 本發明係關於控制有害眞菌及昆蟲之混合物,包括 a)式I之苯乙酸衍生物 R3~ Υζ / 4, Description of the invention (1) The present invention relates to the control of harmful maggots and insect mixtures, including a) phenylacetic acid derivative R3 of formula I

(I) 其中取代基及參數具有下列定義: X 係 noch3、ch〇ch3或chch2 係氧或N R ; R分別各爲氫及CrC4-烷基; 係氰基、硝基、三說甲基、 crc4-烷氧基; 係0、1或2,其中若m係2則R2基可相異; C「C4-烷基、cvcv 鹵烷基、C3-C6- Y R1 R2 m R3 鹵素、CrC4-燒基及 -------^-------裳--- (請先閱讀背面之注音?事項本頁} 訂· 係氫、氰基 環燒基; R4、R6分別各爲氫 CrC1()-烷基 -丨線· 經濟部智慧財產局員工消費合作社印製 C3_C6-味坑基、c2-C1()-晞基 炔基、CrC1G-烷羰基、c2_Ci(r烯羰基、c3_c^炔 基或CrC1(r坑續g盛基’其中這些基可_部份或完 全齒化或可帶有一至三個下列基:氰基、硝基、 羥基、鲦基、胺基、j基、胺羰基、胺硫羰基、 1¾素、C「C6-fe基、c「c6-卣烷基、Ci-CV垸續醯 基、C「C6-烷亞續醯基、c「c6-烷氧基、c「C6-卣 C2-C1(r -4- ‘紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) 520274 A7 -----B7 五、發明說明(2 ) (請先閱讀背面之注意事項本頁) 氧基、CrC6-燒氧羰基、c「c6-燒硫基、CrC6_ 坑胺基、二-C「C6-烷胺基、Crc6-燒胺羰基、二-CVCV烷胺羰基、crc6-烷胺硫羰基、二-CrC6^ 胺硫羰基、C2-C6-晞基、C2-C6-烯氧基、c3-c6-環 基、C3-C0-環烷氧基、雜環基、雜環氧基、芊 基、芊氧基、芳基、芳氧基、芳硫基、雜芳基、 雜芳氧基及雜芳硫基,其中該部份之環基可部份 或完全_化或可帶有一至三個下列基··氰基、硝 基、喪基、銳基、胺基、複基、胺羰基、胺硫羰 基、i 素、crc6-:fe·基、cvc6-卣燒基、cvcv燒 基、CVC6-燒亞續基、c3-C6-環燒基、cv c6-燒氧基、crc6-鹵烷氧基、crC6-烷氧羰基、 cvcv燒硫基、crc6-烷胺基、二-crc6-烷胺基、 CVCV燒胺羰基、二_c「c6-烷胺羰基、c「C6-烷胺 硫談基、二-C「C6-烷胺硫羰基、c2-cv烯基、c2-c0-烯氧基、芊基、芊氧基、芳基、芳氧基、芳硫 基、雜芳基、雜芳氧基、雜芳硫基或C(=NOR7)-An-R8 ; 經濟部智慧財產局員工消費合作社印製 芳基、芳羰基、芳磺醯基、雜芳基、雜芳羰基或 雜芳磺醯基、其中這些基可部份或完全滷化或可 帶有一至三個下列基:氰基、硝基、羥基、巯基、 胺基、羧基、胺羰基、胺硫羰基、画素、Crc6-烷 基、Crc6-鹵烷基、烷羰基、CrC6-烷磺醯 基、crc6-燒亞績酸基、c3-C6-環炫基、CrC6-垸 -5- 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) 520274 A7 B7 五、發明說明(3 ) 氧基、CrC6-鹵烷氧基、CrC6-烷氧羰基、c「c6- 坑石JfL基、CrC6-坑胺基、二-CVCV〗充胺基、 烷胺羰基、二-CrC6-烷胺羰基、CVC6-烷胺硫羰 基、二-CrC6-烷胺硫羰基、C2-C6-烯基、C2-C6-晞 氧基、芊基、芊氧基、芳基、芳氧基、雜芳基、 雜芳氧基或C(=NOR7)-An-R8 ; R5 係氫,(I) The substituents and parameters have the following definitions: X is noch3, choch3, or chch2 is oxygen or NR; R is hydrogen and CrC4-alkyl, respectively; cyano, nitro, tris-methyl, and crc4 -Alkoxy; 0, 1 or 2; where m is 2, then the R2 group may be different; C "C4-alkyl, cvcv haloalkyl, C3-C6- Y R1 R2 m R3 halogen, CrC4- Base and ------- ^ ------- Shang --- (Please read the phonetic on the back? Matters on this page} Order · Department of hydrogen and cyano ring; R4 and R6 are each Hydrogen CrC1 ()-Alkyl- 丨 Line · Printed by C3_C6-Wei Keji, c2-C1 ()-Aminoyl, CrC1G-Alkylcarbonyl, c2_Ci (renecarbonyl, c3_c) ^ Alkynyl or CrC1 (r), where these groups may be partially or fully dented or may carry one to three of the following groups: cyano, nitro, hydroxyl, fluorenyl, amine, j , Amine carbonyl, amine thiocarbonyl, 1¾, C, C6-fe, c, c6-fluorenyl, Ci-CV, fluorenyl, C, C6-alkylidene, c, c6-alkoxy Basic, c "C6- 卣 C2-C1 (r -4- 'paper size applies to China National Standard (CNS) A4 specification (210 X 297 mm) 520274 A7 ----- B7 V. Description of the invention (2) (Please read the precautions on the back page first) Oxygen, CrC6-oxooxycarbonyl, c "c6-thiothio, CrC6_ amine, di-C "C6-alkylamino, Crc6-alkylaminocarbonyl, di-CVCV alkylaminecarbonyl, crc6-alkylaminethiocarbonyl, di-CrC6 ^ aminothiocarbonyl, C2-C6-fluorenyl, C2-C6-alkenyloxy, c3-c6-cyclo, C3-C0-cycloalkoxy, heterocyclyl, heterocyclyl, fluorenyl, fluorenyloxy, aryl, aryloxy, arylthio, heteroaryl, heteroaryloxy And heteroarylthio groups, in which the cyclic group may be partially or completely atomized or may carry one to three of the following groups: cyano, nitro, benzyl, sharp, amine, compound, Amine carbonyl, amine thiocarbonyl, i element, crc6-: fe · group, cvc6-fluorenyl group, cvcv alkyl group, CVC6-alkylene group, c3-C6-cycloalkyl group, cv c6-alkyloxy group, crc6 -Haloalkoxy, crC6-alkoxycarbonyl, cvcvsulfanyl, crc6-alkylamino, di-crc6-alkylamino, CVCV alkylamine carbonyl, di-c "c6-alkylaminecarbonyl, c" C6- Alkylaminothio, di-C6-C6-alkylaminethiocarbonyl, c2-cv alkenyl, c2-c0-enyloxy, fluorenyl, fluorenyloxy, aryl, aryloxy , Arylthio, heteroaryl, heteroaryloxy, heteroarylthio or C (= NOR7) -An-R8; printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, aryl, arylcarbonyl, arylsulfonyl, Heteroaryl, heteroarylcarbonyl or heteroarylsulfonyl, where these groups may be partially or completely halogenated or may carry one to three of the following groups: cyano, nitro, hydroxyl, thiol, amino, carboxyl, aminecarbonyl , Amine thiocarbonyl, pixel, Crc6-alkyl, Crc6-haloalkyl, alkylcarbonyl, CrC6-alkylsulfonyl, crc6-alkylene, c3-C6-cyclohexyl, CrC6-fluoren-5- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 520274 A7 B7 V. Description of the invention (3) Oxygen, CrC6-haloalkoxy, CrC6-alkoxycarbonyl, c "c6- pit Stone JfL group, CrC6-pit amino group, di-CVCV amine group, alkylamine carbonyl group, di-CrC6-alkylamine carbonyl group, CVC6-alkylamine thiocarbonyl group, di-CrC6-alkylamine thiocarbonyl group, C2-C6- Alkenyl, C2-C6-fluorenyloxy, fluorenyl, fluorenyloxy, aryl, aryloxy, heteroaryl, heteroaryloxy or C (= NOR7) -An-R8; R5 is hydrogen,

Ci-C6-fe基、C2-C6-晞基、C2-C6-块基,其中這些 基之烴基可部份或完全自化或可帶有一至三個下 列基:氰基、硝基、·羥基、疏基、胺基、叛基、 胺羰基、胺硫羰基、卣素、Crc6-烷胺羰基、二-CVCV烷胺羰基、crc6-烷胺硫羰基、二-cvcv烷 胺硫羰基、CrC6-烷磺醯基、crC6-烷亞磺醯基、 crC6-烷氧基、CrC6-鹵燒氧基、c「C6-燒氧羰 基、CrC6-烷硫基、crc6-烷胺基、二-C「C6-烷胺 基、c2-c6-晞氧基、c3-cv環燒基、C3-C6-環烷氧 基、雜環基、雜環氧基、芳基、芳氧基、芳基_ Crcv烷氧基、芳硫基、芳基-Crc4_烷硫基、雜 方基、雜芳氧基、雜芳基-C「C4-烷氧基、雜芳硫 基、雜芳基- CrCV燒硫基,其中該部份之環基可 邵份或完全鹵化及/或可帶有一至三個下列基:氰 基、硝基、羥基、巯基、胺基、羧基、胺羰基、 胺石ϋ 基、基、CrCV^:!:完基、CVC6-:fe 績 酿基、CVCV燒亞磺酿基、C3-(V環燒基、CrCV -6 - 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公爱) --------------裝--- - . (請先閱讀背面之注意事項本頁) 1Τ·_ 丨線· 經濟部智慧財產局員工消費合作社印製 520274 A7 五、發明說明(4 經濟部智慧財產局員工消費合作社印製 其中 A η R7 R8 燒氧基、crc6-鹵烷氧基、crc6-烷氧羰基、crc6- 燒硫基、c「c6-烷胺基、二-C「C6-烷胺基、crC6- 燒胺羰基、二-C「C6-烷胺羰基、烷胺硫羰 基、—crc6-祝胺硫羰基、C2-C6-晞基、c2-C6-締 氧基、芊基、苄氧基、芳基、芳氧基、芳硫基、 雜芳基、雜芳氧基、雜芳硫基及C(=NOR7;)-An_ R8 ; n C3-C6·環烷基、C3_C6_環烯基、雜環基、芳基、雜 芳基,其中環基可部份或完全鹵化或可帶有一至 二個下列基:氰基、·硝基、羥基、巯基、胺基、 焱基、胺羰基、胺硫羰基、鹵素、烷基、 C1-C6-鹵烷基、crc6-烷磺醯基、烷亞磺醯 基、C3-C6-環垸基、cvcy完氧基、Ci-Cv _烷氧 基、Crc6-燒氧羰基、C「C6-垸硫基、c「c6•規胺 基、二-crc6-燒胺基、cvcv燒胺談基、二-c「 C6-烷胺羰基、Cl_c6-烷胺硫羰基、二烷胺 石爲致基、C2-C6-烯基、c2-C6-烯氧基、苄基、苄氧 基、芳基、芳氧基、雜芳基及雜芳氧基; 係氧、硫或氮且其中氮帶有氫或K「烷基; 係0或1 ; 係氫或CrC6-烷基且 係氫或CrC6-烷基,— 及其鹽Ci-C6-fe group, C2-C6-fluorenyl group, C2-C6-block group, in which the hydrocarbon group of these groups may be partially or completely self-defined or may carry one to three of the following groups: cyano, nitro, · Hydroxyl, thiol, amine, amide, aminocarbonyl, aminethiocarbonyl, halogen, Crc6-alkylaminecarbonyl, di-CVCV alkylaminecarbonyl, crc6-alkylaminethiocarbonyl, di-cvcv alkylaminethiocarbonyl, CrC6 -Alkylsulfonyl, crC6-alkylsulfinyl, crC6-alkoxy, CrC6-halohaloxy, c6-C6-alkoxycarbonyl, CrC6-alkylthio, crc6-alkylamino, di-C "C6-alkylamino, c2-c6-fluorenyloxy, c3-cv cycloalkyl, C3-C6-cycloalkoxy, heterocyclyl, heterocyclyloxy, aryl, aryloxy, aryl_ Crcv alkoxy, arylthio, aryl-Crc4-alkylthio, heterosquare, heteroaryloxy, heteroaryl-C, C4-alkoxy, heteroarylthio, heteroaryl-CrCV Thio, in which the cyclic group may be partially or fully halogenated and / or may carry one to three of the following groups: cyano, nitro, hydroxy, thiol, amine, carboxyl, aminecarbonyl, aminecarboxanyl , Base, CrCV ^:!: Wanji, CVC6-: fe jiji, CVCV sulfinyl, C3- (V ring CrCV -6-This paper size is applicable to China National Standard (CNS) A4 specification (210 X 297 public love) -------------- install ----(Please read the Note on this page) 1Τ · _ 丨 Line · Printed by the Intellectual Property Bureau of the Ministry of Economic Affairs 'Consumer Cooperatives 520274 A7 V. Description of the invention (4 Printed by the Intellectual Property Bureau of the Ministry of Economic Affairs' Consumer Cooperatives where A η R7 R8 thiol, crc6- Haloalkoxy, crc6-alkoxycarbonyl, crc6-sulfanyl, c "c6-alkylamino, di-C" C6-alkylamino, crC6-alkylaminocarbonyl, di-C "C6-alkylaminecarbonyl , Alkylamine thiocarbonyl, -crc6-aminoamine thiocarbonyl, C2-C6-fluorenyl, c2-C6-associyloxy, fluorenyl, benzyloxy, aryl, aryloxy, arylthio, heteroaryl , Heteroaryloxy, heteroarylthio, and C (= NOR7;)-An_ R8; n C3-C6 cycloalkyl, C3_C6_cycloalkenyl, heterocyclyl, aryl, heteroaryl, among which the cyclic group May be partially or completely halogenated or may carry one to two of the following groups: cyano, nitro, hydroxyl, thiol, amine, fluorenyl, amine carbonyl, amine thiocarbonyl, halogen, alkyl, C1-C6-halo Alkyl, crc6-alkanesulfenyl, alkylsulfinyl, C3-C6-cyclofluorene , Cvcy alkoxy, Ci-Cv_alkoxy, Crc6-carboxycarbonyl, C "C6-fluorenylthio, c" c6 • regamine, di-crc6-carbamine, cvcv alkyl, Di-c "C6-alkylamine carbonyl, Cl_c6-alkylamine thiocarbonyl, dialkylamine stone as a radical, C2-C6-alkenyl, c2-C6-alkenyloxy, benzyl, benzyloxy, aryl, Aryloxy, heteroaryl, and heteroaryloxy; is oxygen, sulfur, or nitrogen and wherein nitrogen bears hydrogen or K "alkyl; is 0 or 1; is hydrogen or CrC6-alkyl and is hydrogen or CrC6-alkane Base, — and its salts

-------------裝--- * - (請先閱讀背面之注意事項本頁) 訂· -線· 經濟部智慧財產局員工消費合作社印製 520274 A7 B7___ 五、發明說明(8 )------------- Installation --- * * (Please read the note on the back page first) Order--Line Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 520274 A7 B7___ V. Invention description (8)

Otsuka; Furacon®,來自 Siapa Chem); IX · CAS RN 1 1 1 988-49-9,俗名:thiacloprid(來自 Bayer之 發展產品); X · Porc· of the 1998 Brighton Conference f,Pests 及Otsuka; Furacon® from Siapa Chem); IX · CAS RN 1 1 1 988-49-9, common name: thiacloprid (developed product from Bayer); X · Porc · of the 1998 Brighton Conference f, Pests and

Diseases’’,Vol. 1,pp. 21-26 (MTI 446,來自 Mitsui);Diseases ’’, Vol. 1, pp. 21-26 (MTI 446 from Mitsui);

Proc. of the Brighton Conference on Pests and Diseases,Proc. Of the Brighton Conference on Pests and Diseases,

Vol. 1,pp· 27-36(CGA 293 343,來自 Novartis) o 由於化合物I之c = C -及c = N -雙鍵,化合物I可由到呈E / z 異構物之混合物而獲得,其可以常規方式(例如結晶或色層 分析)分成各個化合物。 若合成得到異構物混合物,通常不需分離,原因在某些情 形中異構物在碉配或施用期間(如曝光、酸或鹼)可彼此相 互轉化。相似轉化作用亦可發生在施用後如在處理植物, 或有害眞菌或欲控制動物害蟲。 由C = x雙鍵來看,化合物〗之£型異構物係有較佳活性(以 相對於-C^R1之-OCH3或弋h3基爲主構型)。 ,由<(!13)=>^0(:112_雙鍵來看,化合物〗之順式異構物係有 較佳活性(以相對於-OCH2·基之R3基爲主構型)。 於開始之化合物!之定義中,所用之集合性術語常代 列取代基: 齒素·氟、氯、溴及換; k基.1至4、6或丨〇個碳原子之直鏈或支鏈烷基,例如 Cl々燒基,如甲基、乙基、丙1、1-甲基乙基、丁基、i 曱基丙基、2·甲基丙基、1,“二甲基乙基、戊基、甲基丁 . I---- --- * ♦ (請先閱讀背面之注意事項本頁)Vol. 1, pp. 27-36 (CGA 293 343, from Novartis) o Due to the c = C-and c = N-double bonds of compound I, compound I can be obtained as a mixture of E / z isomers, It can be separated into individual compounds in a conventional manner, such as crystallization or chromatography. If a mixture of isomers is synthesized, separation is usually not required, because in some cases the isomers can be converted into each other during compounding or application (such as exposure, acid or base). Similar transformations can also occur after application, such as in the treatment of plants, or harmful fungi or animal pests to be controlled. From the perspective of C = x double bond, the £ type isomer of the compound has better activity (mainly in the -OCH3 or 弋 h3 group relative to -C ^ R1). From the point of view of < (! 13) = > ^ 0 (: 112_double bond, the cis isomer of the compound〗 has better activity (the main configuration is the R3 group relative to the -OCH2 · group) ). In the definition of the compound at the beginning! The collective terms used often list substituents: halides · fluorine, chlorine, bromine, and permutation; k-groups. Straight chain of 1 to 4, 6 or 0 carbon atoms Or a branched alkyl group, such as a methyl group, such as methyl, ethyl, propane 1, 1-methylethyl, butyl, i-propylpropyl, 2. methylpropyl, 1, "dimethyl Ethyl, pentyl, methylbutyl. I ---- --- * ♦ (Please read the precautions on this page first)

It,· --線 -11 - 520274 A7 B7 五、發明說明(9 ) 基、2-甲基丁基、3-甲基丁基、2,二甲基丙基、卜乙基丙 基、己基、1山二甲基丙基、i,2•二甲基丙基、卜甲基戊 基、2-曱基戊基、3-曱基戊基、4_甲基戊基 基…甲基丁基、i,3-二甲基丁基、2,2·二甲:丁甲;丁 2,3-二甲基丁基、3,3_二甲基丁基、卜乙基丁基、厂乙基丁 基' 1,1,2-三甲基丙基、^2-三甲基丙基、丨_乙基小甲基 丙基及1-乙基-2-甲基丙基; i烷基·· 1至6個碳原子之上述直鏈或支鏈烷基,其中這 些基一些或全部之氫原子可由上述之商原子取代,例如Cr Cri貌基’如氣甲基、二氣甲-基、三氣甲基、氟甲基、二 氟甲基、三氟甲基、氯氟甲基、二氣氟甲基、氣二氟甲 基、1-氟乙基、2-氯乙基、2,2-二氟乙基、2,2,2_三氟乙 基、2 -氯-2-氟乙基、2 -氯-2,2-二氟乙基、2,2-二氯氟乙 基、2,2,2-三氟乙基及五氟乙基; ¥烷基:3至6個碳環員之單環烷基,例如環丙基、環丁 基、環戊基及環己基; 烯基:未飽和直鏈或支鏈且具2至6或丨〇個碳原子及於任 何位置上有一雙鍵之烴基,例如c2-C6-烯基如乙烯基、卜丙 烯基、2-丙晞基、1-甲基乙烯基、^丁烯基、2_丁烯基、 3 -丁晞基、1-甲基-1-丙晞基、2-甲基-丨-丙烯基、卜甲基—2-丙烯基、2 -甲基-2-丙烯基、1-戊烯基、2-戊烯基、戊烯 基、4-戊烯基、1-甲基-1-丁烯基、2 -甲基-^丁缔基、3-甲 基小丁烯基、1 -甲基-2-丁烯基-甲基-2-丁烯基、3 -甲基 -2-丁烯基、1 -曱基-3-丁烯基、2 -甲基-3-丁烯基、3 -甲基- 12 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) --------------裝--- * * (請先閱讀背面之注意事項本頁) 訂·· 丨線· 經濟部智慧財產局員工消費合作社印製 520274 A7 ------ -B7 ’ 五、發明說明(1〇 ) 3-丁烯基、1,1_二甲基丙烯基、L2-二曱基_丨_丙烯基、 1,2-二甲基-2-丙埽基、b乙基丙晞基、^乙基丙烯 基、1 -己烯基、2 -己烯基、3 _己晞基、仁己烯基、5 _已烯 基、1-甲基-1-戊烯基、2-甲基4_戊烯基、3_甲基4•戊晞 基、4·甲基-1-戊烯基、丨_甲基戊晞基、甲基戊烯 基、3 -甲基-2-戊烯基、4 -甲基-2-戊晞基、1-甲基-3-戊烯 基、2 -甲基-3-戊烯基、3 -甲基-3-戊烯基、4 -甲基-3-戊烯 基、1 -曱基-4-戊晞基、2 -甲基-4-戊烯基、3 -曱基-4-戊烯 基、4 -甲基-4-戊烯基、ι,ι_二甲基·2-丁烯基、丨,卜二甲基· 3-丁烯基、1,2-二甲基·ι_ 丁晞-基、二甲基丁晞基、 1,2-二甲基-3-丁烯基、l,3-二甲基_1_丁烯基、丨,%二甲基 丁埽基、1,3-二甲基-3-丁晞基、2,2-二甲基-3-丁烯基、2,3-一曱基_卜丁烯基、2,3-二甲基-2-丁烯基、2,3-二甲基-3-丁 埽基、3,3-二甲基-1-丁烯基、3,弘二甲基-2_丁烯基、卜乙基 -1-丁烯基、1 _乙基-2-丁烯基、1 _乙基丁烯基、2 _乙基一 1- 丁晞基、2_乙基-2-丁晞基、2 -乙基-3-丁烯基、1,1,2-三甲 基-2-丙晞基、1-乙基-丨_甲基丙烯基、丨_乙基甲基 丙烯基及1-乙基-2-甲基-2-丙烯基; 炔基:具2至1 0個碳原子及於任何位置有一個三鍵之直鏈 或支鏈之烴基,例如C2-C6-块基如乙炔基、丨-丙炔基、2_丙 炔基、1 - 丁炔基、2 - 丁炔基、3 - 丁炔基、1 -甲基-2-丙炔 基、1-戊块基、2-戊块基、3 -戊炔基、4-戊炔基、1-曱基- 2- 丁炔基、1-甲基-3-丁炔基、2 -甲基-3-丁炔基、3 -甲基-1-丁玦基、1,1-一甲基-2-丙決基、1-乙基-2-丙決基、1-己決 -13- 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) ----------I---裝 i I * 紙 C請先閱讀背面之注音?事項本頁} 訂: -丨線· 經濟部智慧財產局員工消費合作社印製 經濟部智慧財產局員工消費合作社印製 520274 A7 _____ B7 五、發明說明(11 ) 基、2 -己炔基、3 -己炔基、4 -己炔基、5 -己炔基、1-甲基-2-戊炔基、1-甲基-3-戊块基、1-曱基_4-戊炔基、2 -甲基-3-戊炔基、2 -甲基-4-戊炔基、3 -甲基-1 -戊炔基、3 -甲基-4-戊炔基、4 -甲基-1-戊炔基、4 -甲基1戊炔基、丨,^二甲基_ 2-丁炔基、Μ-二甲基-3-丁炔基、ι,2-二甲基-3-丁炔基、 2,2-二甲基-3-丁炔基、3,3-二甲基-1-丁炔基、1-乙基-2-丁 炔基、1-乙基-3-丁炔基、2 -乙基-3-丁炔基及1-乙基-卜甲基 -2-丙炔基; 雜環基或雜環氧基、雜環硫基及雜環胺基·· 3至6員,飽 和或部份未飽和單或多環系雜環,其含1至3個選自氧、氮 及硫之雜原子且其經由氧原子(雜環氧基)、或經由硫原子 (雜環硫基)或經由氮原子(雜環胺基)直接键結至主鏈如2 _四 p夫喃基’彡衣氧乙纟元基’ 3 -四氮ρ夫喃基,2 -四氮p塞吩基, 3 -四氫嘧吩基,2 -吡咯啶基,3 -吡咯啶基,3 -異唠唑淀 基’ 4 -異崎峻淀基,5 -異坐啶基,3 -異邊唑啶基,4 -異 嘧唑啶基,5 -異p塞唑啶基,3 -吡唑啶基,4 -吡唑啶基,5 -毗唑啶基,2 -哼唑啶基,4 -嘮唑啶基,5 -呤唑啶基,2 -嘧 唑啶基,4 -嘧唑啶基,5 -嘧唑啶基,2 -咪唑啶基,4 -咪唑 啶基,1,2,4-嘮二唑啶-3-基,1,2,4-呤二唑啶-5-基,1,2,4-嘧 二。坐啶-3-基,1,2,4-嘧二唑啶-5-基,1,2,4-三唑啶-3-基, 1,3,4-嘮二唑啶-2-基,1,3,4-卩塞二唑啶-2-基,1,3,4-三唑啶-2-基,2,3,-二氫呋喃-2-基,2,3-二氫呋喃-3-基,2,3-二氫 咬喃-4-基,2,3-二氫呋喃-5-基T"2,5-二氫呋喃-2-基,2,5-二氫呋喃-3-基,2,3-二氫嘧吩-2-基,2,3-二氫嘧吩-3-基, -14- 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) --------------裝--- - . (請先閱讀背面之注意事項本頁) 訂· -·線· 經濟部智慧財產局員工消費合作社印製 520274 A7 B7 五、發明說明(12 ) 2.3- 二氫p塞吩-4-基,2,3-二氫p塞吩-5-基,2,5-二氫p塞吩-2-基,2,5-二氫p塞吩-3-基,2,3-二氫吡咯-2-基,2,3-二氫吡咯-3 -基 ’ 2,3 - ^'風 p 比洛-4 -基 ’ 2,3 - ^ — 風峨洛-5 -基 ’ 2,5 -二氯 ρ 比 咯-2-基,2,5-二氫吡咯-3-基,2,3-二氫異噚唑-3-基,2,3-二 氫異哼唑-4-基,2,3-二氫異哼唑-5-基,4,5-二氫異崎唑-3-基,4,5-二氫異吟唑-4-基,4,5-二氫異噚唑-5-基,2,5-二氫 異嘧唑-3-基,2,5-二氫異噻唑-4-基,2,5-二氫異p塞唑-5-基,2,3-二氫異吡唑-3-基,2,3-二氫異吡唑-4-基,2,5-二氫 異吡哇-5-基,4,5-二氫異p比吐-3-基,4,5-二氫異p比峻-4-基,4,5-二氫異p比峻-5-基,2,5·-二氫異p比峻-3-基,2,5-二氫 異吡唑-4-基,2,5-二氫異吡唑-5-基,2,3-二氫吟唑-3-基, 2.3- 二氫ρ号唆-4-基,2,3-二氫p号嗤-5-基,4,5-二氫p号吐-3-基,4,5-二氫呤唑-4-基,4,5-二氫吟唑-5-基,2,5-二氫崎唑-3-基,2,5-二氫喝唑-4-基,2,5-二氫崎唑-5-基,2,3-二氫嘧 唑-2-基,2,3-二氫噻唑-4-基,2,3-二氫噻唑-5-基,4,5-二氫 邊唑-2-基,4,5-二氫4唑-4-基,4,5-二氫哼唑-5-基,2,5-二 氫4唑-2-基,2,5-二氫p塞唑-4-基,2,5-二氫噹唑-5-基,2,3-二氫咪唑-2-基,2,3-二氫咪唑-4-基,2,3-二氫咪唑-5-基, 4,5 - —氮味17坐-2-基’ 4,5-二氮味哇-4 -基’ 4,5-二氯味哇-5-基,2,5-二氫咪唑-2-基,2,5-二氫咪唑-4-基,2,5-二氫咪唑-5 -基’ 2 _嗎17林基’ 3 -嗎p林基’ 2 - "ττ風p比淀基’ 3 - 7T氯p比淀 基,4 -六氫p比啶基,3 -四氫塔畊基,4-四氫嗒畊基,2 -四 氫嘧淀基,4 -四氫喃症基,5 -四氫哺淀基,2 -四氫ρ比口井 基,1,3,5-四氣三畊-2-基,1,2,4-四氫三畊-3-基,1,3-二氫 -15- 本紙?ft尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) --------------裝--- t (請先閱讀背面之注意事項本頁) 訂· 線* 520274 A7 經濟部智慧財產局員工消費合作社印剩π 五、發明說明(13 ) :井2·基’ U-U-基’ 2*·四氫哌喃基,1,3-二氧戊烷-=基,3,4,5,6-四氫…-基’,制·2_基,4h_3小 —开塞井2基,1,1_ 一氧_2,3,4,5-四氫"塞吩-2-基,2H-1,4- 丰幵噻唑-3-基,2H-1 4-笨#啐喵q甘 !,4枣幵τ井_夂基,1,3-二氫哼畊-2-基 及1,3-二噻-2-基; 夕芳基或芳氧基,純基,芳羰基和芳伽基:芳族單環或 夕」衣經基’其直接或經由氧原子(_〇_)(芳氧基)或硫原子⑻ (=基),經由幾基(_co_)(芳鎪基),經由續醯基(_S02_)或 (广續醒基)鍵結到主鏈上,例如,苯基,茶基和菲基,或 苯氧基,萘氧基和菲氧基與對應的羰基和磺醯基等; 雜芳基或雜芳氧基,雜芳硫基,雜芳窥基和雜芳績酿基: 芳族-環或多環基,其除了碳環員外另可含一至四個氮原 子或含-至三個氮原子與一個氧或硫原子或含一個氧或硫 原子者,且係直接地或經由氧原子(_〇_)(雜芳氧基)或經由 硫原子(-S-)(雜芳硫基),經由羰基(_c〇_)(雜芳基羰基)或經 由%Si基(-S〇2_)或(雜芳磺醯基)等鍵結到主鏈上者;例如 -含有一至三個氮原子之五員雜芳基··5員雜芳環基,除碳 原子外可含1至3個氮原子當作環員如2_吡咯基,弘吡= 基,3-吡唑基,4-吡唑基,5-吡唑基,2_咪唑基,4_ 吐基,1,2,4·三唑-3-基及1,3,心三唑-.2-基; - -含1至4個氮原子或1至3個氮原子及丨個硫或氧原子或工 氧或硫原子之5員雜芳基:具5員環之雜芳基,除碳原丁 外,可含1至4個氮原子或1至1個氮原子及丨個硫或氧^ 子或1個氧或硫原子爲環員,例如2 _吱喃基、3 _ p夫喃芙、 咪 個 子 I ί — i _ I I • 0 C請先閱讀背面之注意事項本頁) 訂· 丨線. 16 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) 520274 A7 經濟部智慧財產局員工消費合作社印製 五、發明說明(14 ) 2塞刀基3 - 口塞吩基、2 - p比洛基、3 - ρ比洛基、3 -異口号口坐 基、4-異呤唑基、5·異唠唑基、%異嘧唑基、扣異嘧唑 基5異喧峻基、3 - p比π坐基、4 _ p比峻基、5 _ p比峻基、2 _ 咢坐基4 ·。号咬基、5 -气唑基、2 - 口塞唑基、4 - ττ塞。坐基、 5塞坐基、2-咪。坐基、4-咪吐基、以〆-口号二吱_3-基、 1,3,4-$二峻|基、·噻二唑·3-基、噻二唑 基、丨,2,4_三唑-3_基、1,3,4-哼二唑-2-基、1,3,4_嘧二唑 -2-基、1,3,4-三唑-2-基; _含1至3個氮原子或1個氮原子及/或1個氧或硫原子之苯 並稠合5 -員雜芳基:具5員環之雜芳基,除碳原子外可含 1至4個氮原子或丨至3個氮原子及丨個硫或氧原子爲環 員,且其中兩鄰接之碳環員或1個氮及1個鄰接碳環員可 由丁-1,3-一晞-1,4-二基橋聯; -經由氮鍵結且含丨至4個氮原子之5 _員雜芳基或經由氮鍵 結且含1至3個氮原子之苯並稠合5員雜芳基:具5員環之 雜芳基,除碳原子外可含丨至4個氮原子或丨至3個氮原子 馬環員,且其中兩鄰接碳環員或1個氮及1個鄰接碳環員 可由丁 _ 1,3-一烯- i,4-二基橋聯,此等環經由氮環員中之 -鍵結於主鏈; -含1至3個或1或4個氮原子之6員雜芳基:具6員環之雜芳 基,除碳原子外可含i至3個或i至4個氮原子爲環員,例 如2-吡啶基、3-吡啶基、4_吡啶基、嗒畊基、牝忒畊 基、2 -嘧哫基、4 -嘧啶基、5〕密啶基、2 -吡畊基、i 3 5 三畊-2-基、1,2,4-三畊-3-基及1,2,4,5-四畊-3-基; -17- 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) (請先閱讀背面之注咅?事項 本頁) 裝 訂. 520274 A7 經濟部智慧財產局員工消費合作社印製 、發明說明(15 ) -含1至4個氮原子之苯幷稠合6員雜芳基:6 其中一個相鄰接碳環員可由丁·i,3_二烯·—:衣土, 峻淋、異料L林及如Μ, …基橋聯如 及對應氧、硫、羰基或續醯基。 _基:芳族—環或多環基,其除了碳 — J四個亂原子或含一至三個氮原子與—個氧或—個:子,且係直接地鍵結到主鏈上者。 #、 、術語"部份或完全_化"表示基團中一些或全部氯原子可 被相同或相異如上述鹵素原子替代。有關其生物活性,較佳者係式I之化合物,其中則系〇。 同樣地’較佳者係式I化合物,其中R1係甲基。 此外,較佳者係化合物!,其中R3係氫、氰基 甲基、乙基、1-甲乙基或^。 另外,車父佳者係化合物j,其中R3係甲基。 較佳者係化合物I,其中R3係氰基。 車父佳者係化合物I,其中R3係環丙基。 幸父佳者係化合物I,其中R3係CF3。 車父佳者係化合物I,其中R5係氫、環丙基 乙基、異丙基、未經取代或經取代芳基或雜芳基。 此外,較佳者係化合物j,其中R5係甲基。其中R5係乙基。其中R5係異丙基。其中 1R5係環丙基。 其中R5係CF3。 環丙基 --------------裝--- 一 - (請先閱讀背面之注意事項本頁) 訂· 此外 另外 此外 另外 另外 此外 此外 此外It, ... --line -11-520274 A7 B7 V. Description of the invention (9) group, 2-methylbutyl, 3-methylbutyl, 2, dimethylpropyl, ethylethyl, hexyl, 1 Dimethyl propyl, i, 2 dimethyl propyl, p-methylpentyl, 2-fluorenylpentyl, 3-fluorenylpentyl, 4-methylpentyl ... methylbutyl, i, 3-dimethylbutyl, 2,2 · dimethyl: butyl methyl; butyl 2,3-dimethylbutyl, 3,3-dimethylbutyl, ethyl ethyl, butyl ethyl '1 1,2-trimethylpropyl, ^ 2-trimethylpropyl, 丨 ethyl small methylpropyl and 1-ethyl-2-methylpropyl; i alkyl · 1 to 6 Carbon atom of the above straight or branched alkyl group, in which some or all of the hydrogen atoms of these groups may be replaced by the above quotient atom, such as Cr Criyl group such as methyl, dimethyl, trimethyl , Fluoromethyl, difluoromethyl, trifluoromethyl, chlorofluoromethyl, difluorofluoromethyl, fluorodifluoromethyl, 1-fluoroethyl, 2-chloroethyl, 2,2-difluoro Ethyl, 2,2,2-trifluoroethyl, 2-chloro-2-fluoroethyl, 2-chloro-2,2-difluoroethyl, 2,2-dichlorofluoroethyl, 2,2 , 2-trifluoroethyl and pentafluoroethyl; ¥ alkane Group: monocyclic alkyl group with 3 to 6 carbon ring members, such as cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; Alkenyl: unsaturated straight or branched chain with 2 to 6 or Carbon atom and a hydrocarbon group having a double bond at any position, such as c2-C6-alkenyl such as vinyl, propenyl, 2-propenyl, 1-methylvinyl, butenyl, 2-butene Methyl, 3-butyridinyl, 1-methyl-1-propenyl, 2-methyl- 丨 -propenyl, methyl-2-propenyl, 2-methyl-2-propenyl, 1-pentenyl, 2-pentenyl, pentenyl, 4-pentenyl, 1-methyl-1-butenyl, 2-methyl-butenyl, 3-methyl-butenyl, 1-methyl 2-butenyl-methyl-2-butenyl, 3-methyl-2-butenyl, 1-fluorenyl-3-butenyl, 2-methyl-3-butenyl, 3 -Methyl- 12 This paper size is applicable to China National Standard (CNS) A4 (210 X 297 mm) -------------- install --- * * (Please read the Note on this page) Order ·· 丨 Line · Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 520274 A7 ------ -B7 'V. Description of the invention (1〇) 3-butenyl, 1, 1_ Dimethacryl, L2-di _ 丨 _propenyl, 1,2-dimethyl-2-propenyl, b ethylpropenyl, ^ ethylpropenyl, 1-hexenyl, 2-hexenyl, 3_hexyl Methyl, hexenyl, 5-hexenyl, 1-methyl-1-pentenyl, 2-methyl 4-pentenyl, 3-methyl 4-pentyl, 4-methyl-1 -Pentenyl, 5-methylpentenyl, methylpentenyl, 3-methyl-2-pentenyl, 4-methyl-2-pentenyl, 1-methyl-3-pentene Group, 2-methyl-3-pentenyl, 3-methyl-3-pentenyl, 4-methyl-3-pentenyl, 1-fluorenyl-4-pentenyl, 2-methyl 4-pentenyl, 3-fluorenyl-4-pentenyl, 4-methyl-4-pentenyl, ι, ι-dimethyl · 2-butenyl, 丨, dimethyl · 3-butenyl, 1,2-dimethyl · ι_butylfluorenyl-, dimethylbutylfluorenyl, 1,2-dimethyl-3-butenyl, 1,3-dimethyl_1_butyl Alkenyl, 丨,% dimethylbutytyl, 1,3-dimethyl-3-butytyl, 2,2-dimethyl-3-butenyl, 2,3-monomethyl-butenyl, 2,3-dimethyl-2-butenyl, 2,3-dimethyl-3-butenyl, 3,3-dimethyl-1-butenyl, 3,2-dimethyl-2-butene Methyl, ethyl-1-butenyl, 1-ethyl-2- Alkenyl, 1-ethylbutenyl, 2-ethyl-l-butenyl, 2-ethyl-2-butenyl, 2-ethyl-3-butenyl, 1,1,2-trimethyl- 2-propenyl, 1-ethyl- 丨 _methacryl, 丨 _ethylmethpropenyl, and 1-ethyl-2-methyl-2-propenyl; alkynyl: having 2 to 1 0 Straight or branched hydrocarbon groups with three carbon bonds at any position, such as C2-C6-block groups such as ethynyl, 丨 -propynyl, 2-propynyl, 1-butynyl, 2 -Butynyl, 3-butynyl, 1-methyl-2-propynyl, 1-pentyl, 2-pentyl, 3-pentynyl, 4-pentynyl, 1-fluorenyl -2-butynyl, 1-methyl-3-butynyl, 2-methyl-3-butynyl, 3-methyl-1-butynyl, 1,1-monomethyl-2-propane Base, 1-ethyl-2-propanyl, 1-hexadecane-13- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ---------- I --- Install i I * Please read the phonetic on the back? Matters on this page} Order:-丨 Printed by the Employees 'Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs Printed by the Employees' Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs Printed by 520274 A7 _____ B7 V. Description of the invention (11), 2-Hexynyl, 3 -Hexynyl, 4-hexynyl, 5-hexynyl, 1-methyl-2-pentynyl, 1-methyl-3-pentyl, 1-fluorenyl_4-pentynyl, 2-methyl-3-pentynyl, 2-methyl-4-pentynyl, 3-methyl-1 -pentynyl, 3-methyl-4-pentynyl, 4-methyl-1 -Pentynyl, 4-methyl-1pentynyl, ^ -dimethyl-2-butynyl, M-dimethyl-3-butynyl, i, 2-dimethyl-3-but Alkynyl, 2,2-dimethyl-3-butynyl, 3,3-dimethyl-1-butynyl, 1-ethyl-2-butynyl, 1-ethyl-3-but Alkynyl, 2-ethyl-3-butynyl, and 1-ethyl-bumethyl-2-propynyl; heterocyclyl or heterocyclooxy, heterothio, and heterocyclic amino · 3 to 6 Member, saturated or partially unsaturated mono- or polycyclic heterocyclic ring, which contains 1 to 3 heteroatoms selected from oxygen, nitrogen and sulfur and which is passed through an oxygen atom (heterocyclooxy) or a sulfur atom (hetero Epithio) or directly via nitrogen (heterocyclic amino) Bind to the main chain such as 2-tetra-p-furanyl'synyloxyethylammonium '3-tetraaza-p-furanyl, 2-tetra-nitro-p-sedenyl, 3-tetrahydropyrimyl, 2-pyrrole Pyridyl, 3-pyrrolidinyl, 3-isoxazolidinyl '4-isoisopyridyl, 5-isoisopyridyl, 3-isoimidazolidinyl, 4-isopyrazolidyl, 5- Iso-pyrazolidyl, 3-pyrazolidyl, 4-pyrazolidyl, 5-pyrazolidyl, 2-humidazolyl, 4-oxazolidyl, 5-pyrazolidyl, 2 -Pyrazolidinyl, 4-pyrazolidinyl, 5-pyrazolidinyl, 2-imidazolidyl, 4-imidazolidyl, 1,2,4-pyridazidin-3-yl, 1,2 , 4-pyridazolidin-5-yl, 1,2,4-pyrimidine. Sitazidin-3-yl, 1,2,4-pyrimidazol-5-yl, 1,2,4-triazolidin-3-yl, 1,3,4-amidazolidin-2-yl , 1,3,4-pyridazolidin-2-yl, 1,3,4-triazolidin-2-yl, 2,3, -dihydrofuran-2-yl, 2,3-dihydro Furan-3-yl, 2,3-dihydrofuran-4-yl, 2,3-dihydrofuran-5-yl T " 2,5-dihydrofuran-2-yl, 2,5-dihydro Furan-3-yl, 2,3-dihydropyrimidin-2-yl, 2,3-dihydropyrimidin-3-yl, -14- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) -------------- install ----. (Please read the note on the back page first) Order ·-· Line · Printed by the Consumers ’Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs Preparation 520274 A7 B7 V. Description of the invention (12) 2.3-dihydro p-phenphen-4-yl, 2,3-dihydro p-phenphen-5-yl, 2,5-dihydro p-phenphen-2-yl , 2,5-Dihydrop-phenphen-3-yl, 2,3-dihydropyrrole-2-yl, 2,3-dihydropyrrole-3 -yl '2,3-^' wind p Billot- 4 -yl '2,3-^ — Fengerlo-5 -yl' 2,5-dichloroρ birrol-2-yl, 2,5-dihydropyrrole-3-yl, 2,3-dihydro Isoxazol-3-yl, 2,3-dihydroisoxazol-4-yl, 2,3-dihydroisoxazol-5-yl, 4,5-di Isozazol-3-yl, 4,5-dihydroisoindazol-4-yl, 4,5-dihydroisoxazol-5-yl, 2,5-dihydroisopyrazol-3-yl, 2,5-dihydroisothiazol-4-yl, 2,5-dihydroisopyrazol-5-yl, 2,3-dihydroisopyrazol-3-yl, 2,3-dihydroisopyrazine Azol-4-yl, 2,5-dihydroisopyryl-5-yl, 4,5-dihydroisop-pyridol-3-yl, 4,5-dihydroisop-pyridyl-4-yl, 4,5-dihydroisop ratio Jun-5-yl, 2,5 · -dihydroisop ratio Jun-3-yl, 2,5-dihydroisopyrazol-4-yl, 2,5-di Hydroisopyrazol-5-yl, 2,3-dihydroindazol-3-yl, 2.3-dihydror 唆 -4-yl, 2,3-dihydrop p-5-yl, 4, 5-dihydro p-thol-3-yl, 4,5-dihydropyrazol-4-yl, 4,5-dihydroindazol-5-yl, 2,5-dihydroazazol-3-yl , 2,5-dihydroazol-4-yl, 2,5-dihydroazazol-5-yl, 2,3-dihydropyrazol-2-yl, 2,3-dihydrothiazole-4- Methyl, 2,3-dihydrothiazol-5-yl, 4,5-dihydrorimazol-2-yl, 4,5-dihydro4-zol-4-yl, 4,5-dihydrohumidazole-5 -Yl, 2,5-dihydro4azol-2-yl, 2,5-dihydropetazol-4-yl, 2,5-dihydrodanazol-5-yl, 2,3-dihydroimidazole -2-yl, 2,3-dihydroimidazol-4-yl, 2,3-dihydroimidazol-5-yl, 4,5-nitros 17-syl-2-yl '4,5-diazine -4 -yl '4,5-dichloroamiwa-5-yl, 2,5-dihydroimidazol-2-yl, 2,5-dihydroimidazol-4-yl, 2,5-dihydroimidazol- 5-radical '2 _ 17 lyme' 3-morphine lyme '2-" ττ wind p ratio yodo' 3-7T chloro p ratio yodo, 4-hexahydro p ratio pyridyl, 3-tetra Hydrogen tower, 4-tetrahydrodaphthyl, 2-tetrahydropyrimidyl, 4-tetrahydropyranyl, 5-tetrahydropyridyl, 2-tetrahydroρ ratio wells, 1, 3 , 5-tetrakis-three-cultivation-2-based, 1,2,4-tetrahydro-three-cultivation-3-based, 1,3-dihydro-15- This paper's? Ft scale applies to China National Standard (CNS) A4 specifications ( 210 X 297 mm) -------------- install --- t (please read the precautions on the back page first) Order · Line * 520274 A7 Employee Consumer Cooperative of Intellectual Property Bureau, Ministry of Economic Affairs Printed π V. Description of the invention (13): Well 2 · based 'UU-based' 2 * · tetrahydropiperanyl, 1,3-dioxolane ==, 3,4,5,6-tetra Hydrogen ...- based ', 2 · base, 4h_3 small—Kaisaijing 2 base, 1,1_ monooxy_2,3,4,5-tetrahydro " sephen-2-yl, 2H-1, 4-Hydroxythiazol-3-yl, 2H-1 4-benzy # 啐 喵 q 甘!, 4 Jujube τ well_stilbyl, 1,3-dihydrogen-2-yl and 1,3-di Thia-2-yl Aryloxy, pure, arylcarbonyl, and arylgalanyl: aromatic monocyclic or cyclamyl 'which is directly or via an oxygen atom (_〇_) (aryloxy) or a sulfur atom (= yl), Bonded to the main chain via several groups (_co_) (arylfluorenyl), via continyl (_S02_) or (broadenyl), for example, phenyl, theyl and phenanthryl, or phenoxy, naphthalene Oxy and phenanthryloxy groups and corresponding carbonyl and sulfonyl groups, etc .; heteroaryl or heteroaryloxy, heteroarylthio, heteroaryl and heteroaryl groups: aromatic-ring or polycyclic groups, In addition to carbon ring members, it may contain one to four nitrogen atoms or-to three nitrogen atoms and one oxygen or sulfur atom or one oxygen or sulfur atom, and is directly or via an oxygen atom (_〇_) ( (Heteroaryloxy) or via a sulfur atom (-S-) (heteroarylthio), via a carbonyl (_c〇_) (heteroarylcarbonyl) or via a Si group (-S〇2_) or (heteroarylsulfonate) Fluorenyl) and other bonds to the main chain; for example-five-membered heteroaryl group containing one to three nitrogen atoms · 5-membered heteroaryl ring group, in addition to carbon atoms may contain 1 to 3 nitrogen atoms as a ring Members such as 2-pyrrolidinyl, pyrimidine = yl, 3-pyrazolyl, 4 -Pyrazolyl, 5-pyrazolyl, 2-imidazolyl, 4-tyl, 1,2,4 · triazol-3-yl and 1,3, cardiac triazole-.2-yl;--containing 1 5-membered heteroaryl group with 4 to 4 nitrogen atoms or 1 to 3 nitrogen atoms and 1 sulfur or oxygen atom or working oxygen or sulfur atom: a heteroaryl group having a 5-membered ring, which may contain 1 To 4 nitrogen atoms or 1 to 1 nitrogen atom and 1 sulfur or oxygen atom or 1 oxygen or sulfur atom as a ring member, for example, 2 _ sulphanyl, 3 _ p fulanf, imi son I ί — i _ II • 0 C Please read the notes on the back page first) Order · 丨 Line. 16 This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) 520274 A7 Employees ’Consumption of Intellectual Property, Ministry of Economic Affairs Printed by the cooperative V. Description of the invention (14) 2 stilbyl 3-orthophenidyl, 2-p-pyrrolyl, 3-p-pyrrolyl, 3-iso-slogan succinyl, 4-isopyrazolyl, 5 · isoxazolyl,% isopyrazolyl, 5isopyrazolyl, 3-p ratio pi group, 4 _ p ratio group, 5 _ p ratio group, 2 _ group Base 4 ·. No. octyl, 5-oxazolyl, 2-xazosyl, 4-ττ plug. Sitting base, 5 plug sitting base, 2-mi. Sorryl, 4-imidyl, dioxan-3-yl, 1,3,4- $ dijunyl, thiadiazol-3-yl, thiadiazolyl, 2 ,, 2, 4-triazol-3-yl, 1,3,4-humidazol-2-yl, 1,3,4-pyrimidazol-2-yl, 1,3,4-triazol-2-yl; _Benzo-fused 5-membered heteroaryl group containing 1 to 3 nitrogen atoms or 1 nitrogen atom and / or 1 oxygen or sulfur atom: a heteroaryl group having a 5-membered ring, which may contain 1 in addition to carbon atoms To 4 nitrogen atoms or 丨 to 3 nitrogen atoms and 丨 sulfur or oxygen atoms are ring members, and two adjacent carbocyclic members or 1 nitrogen and 1 adjacent carbocyclic members may be d-1,3-a晞 -1,4-diyl bridge;-5-membered heteroaryl group bonded via nitrogen and containing 丨 to 4 nitrogen atoms or benzo-fused 5-nitrogen bonded and containing 1 to 3 nitrogen atoms 5 Heteroaryl: a heteroaryl with a 5-membered ring, in addition to carbon atoms, may contain 丨 to 4 nitrogen atoms or 丨 to 3 nitrogen atoms, and two adjacent carbocyclic members or 1 nitrogen and 1 Adjacent carbocyclic members can be bridged by butane-1,3-monoene-i, 4-diyl, these rings are bonded to the main chain via-of nitrogen ring members;-containing 1 to 3 or 1 or 4 6-membered heteroaryl with 5 nitrogen atoms: heteroaryl with 6-membered ring Group, in addition to carbon atoms, may contain i to 3 or i to 4 nitrogen atoms as ring members, such as 2-pyridyl, 3-pyridyl, 4-pyridyl, daphyl, stilbyl, 2- Pyrimidinyl, 4-pyrimidinyl, 5] pyrimidinyl, 2-pyridinyl, i 3 5 triphen-2-yl, 1,2,4-trigon-3-yl and 1,2,4, 5-four-cultivation-3-based; -17- This paper size applies to Chinese National Standard (CNS) A4 (210 X 297 mm) (Please read the note on the back? Matters page first) Binding. 520274 A7 Ministry of Economic Affairs Printed by the Intellectual Property Bureau, Consumer Cooperatives, Invention Description (15)-Benzene condensed with 1 to 4 nitrogen atoms, 6-membered heteroaryl group: 6 One of the adjacent carbon ring members can be Ding · i, 3_ 二Ethylene ---: clay, leaching, foreign materials, L, etc., such as M, ... and bridging, such as corresponding oxygen, sulfur, carbonyl or fluorenyl. _ Group: aromatic-ring or polycyclic group, in addition to carbon-J four chaotic atoms or containing one to three nitrogen atoms and-one oxygen or-: child, and is directly bonded to the main chain. #, And the term " partially or completely " means that some or all of the chlorine atoms in the group may be replaced by the same or different halogen atoms as described above. With regard to its biological activity, the compounds of formula I are preferred, and 0 is preferred. Likewise, 'preferred' is a compound of formula I, wherein R1 is methyl. In addition, the preferred ones are compounds! Where R3 is hydrogen, cyanomethyl, ethyl, 1-methylethyl or ^. In addition, car cheer is compound j, of which R3 is methyl. Preferred is compound I, wherein R3 is cyano. Chevrolet is compound I, of which R3 is cyclopropyl. Fortunately, the father is Compound I, and R3 is CF3. Chevrolet is a compound I, wherein R5 is hydrogen, cyclopropylethyl, isopropyl, unsubstituted or substituted aryl or heteroaryl. In addition, preferred is compound j, in which R5 is methyl. R5 is ethyl. Among them, R5 is isopropyl. Among them, 1R5 is cyclopropyl. Among them, R5 is CF3. Cyclopropyl -------------- Packing --- One-(Please read the precautions on the back page first) Order

較佳者係化合物I 較佳者係化合物j 較佳者係化合物j 較佳者係化合物I 18- 本紙張尺度適用中國國家標準(CNS)A4規格(21〇 X 297公釐) i線. 甲基 520274The better one is compound I, the better one is compound j, the better one is compound j, and the better one is compound I. 18- This paper size is applicable to Chinese National Standard (CNS) A4 specification (21〇X 297 mm) i-line. A Base 520274

五、發明說明(16 ) 另外,車乂佳者係化合物J,其中R5係未經取代或經取代芳 基或雜芳基。 、另外’、較佳者係化合物!,其中R5係未經取代或經取代吡 咬基、嘧啶基、吡畊基、嗒畊基或三畊基。 另外,,較佳者係化合物J,其中R5係未經取代或經取代呋 喃基、P塞吩基或P比P各基。 此外,較佳者係化合物!,其中R5係未經取代或經取代嘮 唑基、嘧唑基、異噚唑基、異嘧唑基、吡唑基或嘧唑基。 一此外,較佳者係化合物!,其中R5係未經取代或經取代噚 二吐基、嘍二唑基或三唑基。· 另外,較佳者係化合物!,其中R5係苯基,其未經取代或 帶有一或二個下列基··硝基、氰基、羥基、胺基、胺羰 ,月文&焱基、鹵素、c「C4-垸基、crC4-_烷基、crc4-垸 氧基CrCr鹵烷氧基、cvcv烷胺基、二烷胺基、 Ci C:4垅績醞基、crC4_烷氧羰基、胺羰基、或二_ Crc4-烷胺羰基。 另外,較佳者係化合物Ϊ,其中R4係氫、Ci_C6_烷基、C2_ Q-缔基、cvcv炔基、烯丙基、芳烷基、雜芳烷基、芳氧 燒基、雜芳氧烷基、芳基或雜芳基。 另外,較佳者係化合物I,其中R4係Ci_c「烷基。 另外較佳化合物I係揭示於W 〇 9 7 /15,5 5 2。 匕含^於本發明之混合物之化合物π具有對抗廣泛植物病原性 眞菌,尤其是來自子囊菌綱、半一知菌綱、薄狀菌綱及擔子 菌綱之良好活性。 -19- 冬紙張尺度過用中國國家標準(CNS)A4規格(210 X 297公爱) --------------裝--- < * (請先閱讀背面之注意事項寫本頁) 訂: —線· 經濟部智慧財產局員工消費合作社印製 520274 A7 B7 五、發明說明(17 ) 彼等對控制各種作物如棉花、蔬菜(例如黃瓜、豆類、蕃 %、馬铃薯及葫蘆)、大麥、青草、燕麥、香薦、咖啡、玉 米、水果、稻米、黑麥、大豆、葡萄、小麥、觀賞植物、 甘蔗及多種種子上之許多眞菌特別重要。 其特別適用於防治下列植物致病性眞菌:穀類之禾白粉菌 (Erysiphe graminis),葫蘆之二孢白粉菌(以㈣咖 cichoraceamm)及單絲殼(Sphaerotheca fuHginea),蘋果之白 叉絲單囊殼(Podosphaera leucotricha),葡萄之葡萄鉤絲殼 (Unciniila necator),穀類之柄銹菌(Puccinia species)物種, 棉花、稻及草地之絲殼菌(Rhizoctonia species)物種,穀類 及甘蔑之黑粉菌(Ustilago species)物種,蘋果之蘋果黑星菌 (Venturia inaequalis)(瘡痂病),穀類之長蠕孢 (Helminthosporium species)物種,小麥之穎枯殼針孢 (Septoria nodorum),草莓、蔬菜、裝飾性植物及葡萄之灰 萄萄孢(Botrytis cinerea)(灰黴),落花生之落花生尾孢 (Cercospora arachidicola),小麥及大麥之假小尾孢 (Pseudocercosporella herpotrichoides),稻之稻痕菌 (Pyriculada oryzae),馬鈴薯及蕃茄之致病疫黴(Phytophthora infestans) ’葡萄之葡萄生單轴徽(Plasmopara viticola),蛇麻 草及胡瓜之假霜徵(Pseudoperonospora species)物種,蔬菜 及水果之鏈格孢(Alternaria species)物種,香蔑之球腔菌 (Mycosphaerella species)物種及鐮孢(Fusarium)及輪枝孢 (Verticillium)物種。 式11至X I之化合物用於控制昆蟲、物蛛類及線蟲類之動 -20 - 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) --------------裝—— 秦 - (請先閱讀背面之注意事項本頁) 訂· 線· 經濟部智慧財產局員工消費合作社印製 520274 A7 B7 五、發明說明(18 ) 物害蟲。彼等可用於作物保護及衛生學,貯存產物供控制 動物害蟲。尤其,彼等適用控制下列動物害蟲: 比蟲σ蟲包括’蝶目(鱗翅目)例如小地蚕、黃地老虎、 阿拉巴馬黏蟲(Alabama argiUacea)、黎豆夜蛾、韻實巢 峨、丫紋夜蛾、松尺蠖、鼠灰捲蛾;Capua miculana、 Cheimatobia brumata、雲杉捲葉蛾、西方雲杉捲葉蛾、 美洲黏蟲、Crocidolomia binotalis、蘋果貴峨、歐洲松毛 蟲、瓜野螟、巨座玉米螟、埃及金鋼鑽、小玉米螟、 Eupoecilia ambiguella、Evetria b〇uliana、粒膚地老虎、 大蠟螟、李小食心蟲、梨小食心蟲、棉鈐蟲、美洲菸夜 蛾、玉米穗夜蛾、菜螟、Hibernia def〇liaria、美國白 蛾、蘋果巢蛾、番茄貴蛾、鐵杉尺蠖、甜菜夜蛾、咖啡 二占 /曰蛾、旋紋潛葉蛾、Lithocolletis blancardella、 Lobesia botrana、黃綠條螟、舞毒蛾、僧尼毒蛾、窄翅 潛葉蛾、天幕毛蟲、甘藍夜蛾、〇rgyia pseud〇tsugate、 臥洲玉米螟、pan〇hs flammea、紅鈴蟲、馬铃薯塊莖 蛾、柑橘潛夜蛾、大菜粉蠓、苜藉綠夜蛾、piatyn〇ta stultana、小菜蛾、橘花巢蛾、油脂巢蛾、pr〇denia surna、黃條黏蟲、大豆夜蛾、松梢捲葉蛾、Scr〇bipai㈧ absoiuta、大螟、葡萄長鬍捲葉峨、草地黏蟲、埃及棉捲 蟲、斜蚊夜蛾、Thaumatop0ea pityocampa、櫟綠捲葉 峨、粉紋夜蛾、及雲杉小捲葉蛾; •甲蟲目(鞘翅目)例如AgrTlus sinuatus、具條叩甲、 Agdotes 〇bScurus、野棉象甲、蘋果花象甲、At〇maria -21 - 本紙張尺度適用中國國豕準(CNS)A4規格(210 X 297公爱) .I — — — — — — — — — — — * I I (請先閱讀背面之注意事項本頁) 訂· 線. 經濟部智慧財產局員工消費合作社印製 520274 A7 B7_____ 五、發明說明(19 ) linearis、大松小膏、甜菜龜甲、豆葉甲、甘藍莢象甲、 Ceuthorrhynchus napi、甜菜脛跳甲、草金針蟲、天門冬 十二星葉甲、雲杉紅翅小蠹、長角葉甲、十二星瓜葉 甲、玉米根葉甲、墨西哥豆瓢蟲、草跳甲、Eutinobothms brasiliensis、Hylobius abietis、埃及苜藉象甲、苜稽葉象 甲、Lema bilineata、Lema melanopus、馬铃薯甲蟲、甜 菜金針蟲、稻象甲、Melanotus communis、Meligethes aeneus、Melolontha hippocastani、I思角金龜、稻負泥 蟲、Otiorrhynchus sulcatus、Otiorrhynchus ovatus、耳鋼 猿葉蟲、庭園麗繩、Phyllophaga sp·,油菜蘭跳甲、蒸菁 淡足跳曱、黃曲條跳甲、日本麗金龜、Psylliodes napi、 錯综小蠹、石碗豆葉象甲、以及蚕豆象、碗豆象、 Bruchus lends、谷象、草竊蠹、銀(胸)谷盜、谷蠹、米 象、赤擬谷盜、谷斑皮蠹及Sitona lineatus,Sitophilus granaria ; • 雙翅目例如埃及斑紋,維克斯斑蚊,Anastrepha ludens, Anopheles maculipennis, Ceratitis capitata, Chrysomya bezziana, Chrysomya hominivorax, Chrysomya macellaria Contarinia sorghicola,Cordylobia anthropophaga,Culex pipiens, Dacus cucurbitae, Dacus oleae, Dasineura brassicae, Fannia canicularis, Gasterophilus intestinalis, Glossina morsitans,Haematobia irritans,Haplodiplosis equestris, Hylemyia platura,Hypoderma lineata, Liriomyza sativae, Liriomyza trifolii, Lucilia cuprina, Lucilia sericata, Lycoria -22- 本紙張尺度中_家標準(CNS)A4規格(210>< 297公 --------------^--- . - (請先閱讀背面之注意事項本頁) 訂‘ --综· 經濟部智慧財產局員工消費合作社印製 520274 經濟部智慧財產局員工消費合作社印製 A7 ___B7___ 五、發明說明(2〇 ) pectoralis, Mayetiola destructor, Musca domestica, Muscina stabulans, Oestrus ovis? Oscinella frit, Pegomya hysocyami, Phorbia antiqua, Phorbia brassicae, Phorbia coarctata, Rhagoletis cerasi, Rhagoletis pomonella, Tabanus bovinus, Tipula oleracea and Tipula paludosa 0 •纓翅目,例如草褐薊馬、苜蓿薊馬、花薊馬、小麥皮薊 馬、橘實薊馬、稻薊馬、Thrips palmi及棉薊馬; • 膜翅目例如新疆菜葉蜂、Atta cephalotes、Atta sexdens、 德克薩斯洲切葉蛾、Hoplocampa minuta、韻實葉蜂、阿 根廷蟻、廚蟻、火蟻、外引紅火蟻及黑火蟻; •異翅亞目之目例如喜綠蝽、多毛長蝽、草黑斑盲蝽、棉 紅虫春、Dysdercus intermedius、Eurygaster integriceps、 棉褐蟢、葉足緣蝽、豆莢盲蝽、牧草盲蝽(Lygus lineolaris)、牧草盲蝽(Lygus pratensis)、稻綠墙、甜菜擬 網蝽、Solubea insularis及Thyanta perditor ; •同翅亞目之目例如Acyrthosiphon onobrychis、婉豆虫牙、 落葉松球虫牙、紅圓价、Aphidula nasturtii、蚕豆虫牙、棉 蚜、蘋果蚜、馬鈴薯長鬍蚜、粉虱、薊短尾蚜、甘藍 虫牙、Dalbulus maid is 、Dreyfus ia nordmannianae 、 Dreyfusia piceae、Dysaphis radicola、蚕豆微葉蟬、蘋果 綿蚜、稻灰飛虱、麥長管蚜、大戟長管蚜、薔薇長管 蚜、蚕豆條尾蚜、薔薇麥蚜、桃(赤)蚜、櫻桃黑瘤額 虫牙、黑尾葉輝、稻褐飛SL、蔑飛鼠、Phorodon humuli、 橘粉蚧、蘋木虱、梨黃木虱、玉米縊管蚜、油灰蚧、麥 -23- 本紙?長尺度適用中國國家標準(CNS〉A4規格(210 X 297公釐) --------------裝--- - * (請先閱讀背面之注意事項本頁) . -線· 經濟部智慧財產局員工消費合作社印製 520274 A7 B7______ 五、潑^月說明(21 ) 二叉蚜、白背飛虱、橘二叉蚜、麥粉虱、溫室白粉虱及 葡萄根瘤蚜; •白蟻目(等翅目)例如 Calotermes flavicollis、Leucotermes flavipes、Reticulitermes lucifugus及Termes natalensis ; •直翅目例如歐洲螻蛄、西藏飛禮、雙帶蚱猛、赤腿蚱 蜢、墨西哥蚱蜢、遷徒蚱蜢、洛磯山蚱蜢、紅翅蝗、美洲 蚱猛、Schistocerca peregrina、Stauronotus maroccanus、 荒地蚱猛、以及家蟋蟀、東方排蠊、德國小蠊及美洲大 蠊; •蛛形網之目如植食性癭蜗如番茄葉刺皮癭蜗、蘋刺癭 虫罱、Brevipalpus phoenicis、苜蓿苔虫茜、鶴耳木歷東方葉 蜗、德克薩斯州橘眞葉虫禹、Eriophyes sheldoni、草地小 瓜蜗、蘋果紅换蛛、橘全瓜蜗、橘銹蜗、測多食蚨線 虫禹、朱砂葉蜗、Tetranychus kanzawai、太平洋紅葉蜗、 線葉虫禹、喙碑如美洲花蜱、Amblyomma variegatum、波 斯隱嗓碑、具環方頭蜱、Boophilus decoloratus、微小失 蜱、Dermacentor silvarum、Hyalomma truncatum、羊硬 蜱、Ixodes rubicundus、Ornithodorus moubata、耳殘味 蜱、Rhipicephalus appendiculatus、Rhipicephalus evertsi、 Sarcoptes scabiei、Tetranychus cinnabarinus、Tetranychus kanzawai、Tetranychus pacificus、Tetranychus telarius 及 Tetanychus urticae ; •線蟲綱例如根結線蟲例如馬#根線蟲、花生根結線蟲及 棉花根線蟲,形成包囊線蟲例如Globodera rostochiensis、 -24- 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) --------------裝—— - - (請先閱讀背面之注意事項本頁) 訂· •線- 520274 A7 B7 經濟部智慧財產局員工消費合作社印製V. Description of the invention (16) In addition, the best car is the compound J, in which R5 is an unsubstituted or substituted aryl or heteroaryl. , In addition, the better ones are compounds! , Where R5 is unsubstituted or substituted pyridyl, pyrimidinyl, pyridyl, daphyl or trigyl. In addition, preferred is compound J, in which R5 is an unsubstituted or substituted furanyl group, a pthiophene group, or each group of P to P. In addition, the preferred ones are compounds! , Wherein R5 is unsubstituted or substituted oxazolyl, pyrazolyl, isoxazolyl, isopyrazolyl, pyrazolyl or pyrazolyl. In addition, the better ones are compounds! , Wherein R5 is unsubstituted or substituted fluorenyl dithiol, fluorenediazole, or triazolyl. · In addition, preferred compounds! , Where R5 is phenyl, which is unsubstituted or has one or two of the following groups: nitro, cyano, hydroxy, amine, amine carbonyl, & fluorenyl, halogen, c , CrC4-_alkyl, crc4-fluorenyloxyCrCr haloalkoxy, cvcv alkylamino, dialkylamino, Ci C: 4-methylamino, crC4-alkoxycarbonyl, aminecarbonyl, or di_Crc4 -Alkylamine carbonyl. In addition, compounds Ϊ are preferred, in which R4 is hydrogen, Ci_C6_alkyl, C2_Q-alkenyl, cvcv alkynyl, allyl, aralkyl, heteroaralkyl, aryloxycarbon. Group, heteroaryloxyalkyl group, aryl group or heteroaryl group. In addition, compound I is preferred, in which R4 is Ci_c "alkyl. In addition, compound I is disclosed in WO 9 7/15, 5 5 2 The compound π contained in the mixture of the present invention has good activity against a wide range of phytopathogenic fungi, especially from the ascomycetes, semi-monophyte, thin-form and basidiomycetes. -19- Winter Paper size used Chinese National Standard (CNS) A4 specification (210 X 297 public love) -------------- install --- < * (Please read the notes on the back first to write this Page) Order: —Line · Economy Printed by the Intellectual Property Bureau's Consumer Cooperatives 520274 A7 B7 V. Description of the Invention (17) They control various crops such as cotton, vegetables (such as cucumbers, beans, rice, potatoes and gourds), barley, grass, oats, Fragrant, coffee, corn, fruit, rice, rye, soybeans, grapes, wheat, ornamental plants, sugar cane and many seeds are particularly important. It is particularly suitable for controlling the following phytopathogenic fungi: cereals Erysiphe graminis, Erysiphe graminis (cichoraceamm) and monofilament shell (Sphaerotheca fuHginea), Podsphaera leucotricha of apple, Unciniila of grape necator), Puccinia species of cereals, Rhizoctonia species of cotton, rice and grass, cereals and Ustilago species of apple Venturia inaequalis (Scabies), Helminthosporium species of cereals, Septoria nodorum of wheat, strawberry Botrytis cinerea (Botrytis cinerea) of vegetables, decorative plants and grapes, Cercospora arachidicola, Pseudocercosporella herpotrichoides of wheat and barley, Pyriculada of rice oryzae), Phytophthora infestans' Plasmopara viticola of grapes, pseudoperonospora species of hops and courgette species, Alternaria of vegetables and fruits ( Alternaria species), Mycosphaerella species and Fusarium and Verticillium species. The compounds of formula 11 to XI are used to control the movement of insects, spiders and nematodes. -20-This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) --------- ----- Equipment—— Qin- (Please read the note on the back page first) Order · Thread · Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 520274 A7 B7 V. Description of the invention (18) Pests. They can be used for crop protection and hygiene, and store products for controlling animal pests. In particular, they are suitable for controlling the following animal pests: The worms σ include the order of the butterfly order (Lepidoptera) such as small silkworm, yellow tiger, Alabama argiUacea, Spodoptera litura, and Rhizoma , Spodoptera frugiperda, Pine loopworm, Rat gray roll moth; Capua miculana, Cheimatobia brumata, Spruce Leaf Roller Moth, Western Spruce Leaf Roller Moth, American armyworm, Crocidolomia binotalis, Apple Guiae, European Pine Caterpillar, Cucurbita spp. Corn borer, Egyptian gold diamond, small corn borer, Eupoecilia ambiguella, Evetria b〇uliana, grained tiger, large wax owl, Prunus beetle, Pear beetle, cotton budworm, Spodoptera frugiperda, Corn earworm , Cabbage magpie, Hibernia defolia, American white moth, apple nest moth, tomato nori moth, hemlock hemiptera, beet armyworm, coffee dice / moth, spiny leaf moth, Lithocolletis blancardella, Lobesia botrana, yellow-green stripe Pupae, Gypsy moth, Monk poisonous moth, Narrow-winged leaf miner, Celestial caterpillar, Cabbage night moth, 〇rgyia pseud〇tsugate, Wozhou corn borer, pan〇hs flammea, Red bollworm, Potato block Stem moth, Citrus nocturnal moth, Plutella xylostella, Spodoptera frugiperda, piatyn〇ta stultana, Plutella xylostella, Orange flower moth, Grease moth, prOdenia surna, Yellow-striped slimeworm, Spodoptera exigua, Pine Leaf-roller moth, Scrobipai㈧ absoiuta, Great cockroach, Grapegrass leafgrass, Grassland armyworm, Egyptian cotton leafworm, Spodoptera litura, Thaumatop0ea pityocampa, Oak leafleaf, Spodoptera litura, and Spruce Leaf curl moth; • Beetle order (Coleoptera) such as AgrTlus sinuatus, Striped beetle, Agdotes 〇bScurus, wild cotton weevil, apple flower weevil, At〇maria -21-This paper size applies to China National Cricket Standard (CNS) A4 Specifications (210 X 297 Public Love) .I — — — — — — — — — — — * II (Please read the notes on the back page first) Order and line. Printed by the Intellectual Property Bureau of the Ministry of Economic Affairs and Consumer Cooperatives 520274 A7 B7_____ 5. Description of the invention (19) linearis, large pine ointment, beet tortoise shell, bean leaf beetle, kale pod weevil, Ceuthorrhynchus napi, beet tibia beetle, grass gold needle beetle, asparagus twelve star leaf beetle, spruce red wing Barberry, long-horned leaf beetle, twelve Melon leaf beetle, corn root beetle, mexican bean ladybug, grass beetle, Eutinobothms brasiliensis, Hylobius abietis, Egyptian alfalfa weevil, alfalfa leaf weevil, Lema bilineata, Lema melanopus, potato beetle, beet gold needle, rice Weevil, Melanotus communis, Meligethes aeneus, Melolontha hippocastani, I horn beetle, rice worm, Otiorrhynchus sulcatus, Otiorrhynchus ovatus, eared steel ape leaf worm, garden beetle, Phyllophaga sp Foot jumping cricket, yellow stripe jumper, Japanese beetle, Psylliodes napi, intricate small pheasant, stone bowl bean leaf weevil, and broad bean, bowl bean, Bruchus lends, valley elephant, grasshopper, silver (chest) valley Pirates, glutinous rice owls, rice elephants, red phoenix pitworms, pitworms, and Sitona lineatus, Sitophilus granaria; • Diptera such as Egyptian spotted mosquitoes, Anopheles mosquitoes, Anastrepha ludens, Anopheles maculipennis, Ceratitis capitata, Chrysomya bezziana, Chrysomya hominivorax, Chrysomya macellaria Contarinia sorghicola, Cordylobia anthropophaga, Culex pipiens, Dacus cuc urbitae, Dacus oleae, Dasineura brassicae, Fannia canicularis, Gasterophilus intestinalis, Glossina morsitans, Haematobia irritans, Haplodiplosis equestris, Hylemyia platura, Hypoderma lineata, Liriomyza sativae, Liriomyza trifolii, Lucilia cup, Lucilia cup Home Standard (CNS) A4 Specification (210 > < 297 Male -------------- ^ ---.-(Please read the Precautions on the back page first) Order '-Comprehensive · Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 520274 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs A7 ___B7___ V. Invention Description (2〇) pectoralis, Mayetiola destructor, Musca domestica, Muscina stabulans, Oestrus ovis? Oscinella frit, Pegomya hysocyami, Phorbia antiqua, Phorbia brassicae, Phorbia coarctata, Rhagoletis cerasi, Rhagoletis pomonella, Tabanus bovinus, Tipula oleracea and Tipula paludosa 0 • Pteroptera, such as grass brown thrips, alfalfa thrips, flower thrips, wheat thrips, Orange thrips, rice thrips, Thrips palmi and cotton thrips; • Hemiptera such as Xinjiang leaf bee, Atta cephalotes, Atta sexdens, Texas leaf-cutting moth, Hoplocampa minuta, leafhopper, Argentine ant, kitchen ant, fire ant, exogenous red fire ant and black fire ant; Orders of Heteroptera, such as the green magpie, hairy long pheasant, black-spotted pheasant, cotton red spring, Dysdercus intermedius, Eurygaster integriceps, cotton brown magpie, leaf foot magpie, pod pod magpie, forage maggot (Lygus lineolaris), Lygus pratensis, rice green wall, beet mimicry, Solubea insularis, and Thyanta perditor; • Homoptera such as Acyrthosiphon onobrychis, pea tooth, larch ball tooth, red round valance, Aphidula nasturtii, broad bean worm tooth, cotton aphid, apple aphid, potato aphid, whitefly, thistle shorttail aphid, cabbage worm tooth, Dalbulus maid is, Dreyfus ia nordmannianae, Dreyfusia piceae, Dysaphis radicola, broad bean micro leafhopper, apple cotton aphid, Rice planthopper, Aphis gossypii, Aphis gossypii, Aphis gossypii, broad bean aphid, Aphis gossypii, peach (red) aphid, cherry melanoma frontal tooth, Tail leaf hui, rice brown fly SL, squirrel fly squirrel, Phorodon humuli, orange powder pupae, apple psyllid, pear yellow psyllid, corn borer aphid, putty pupae, wheat-23-this paper? Long scales are applicable to Chinese national standards (CNS> A4 Specifications (210 X 297 mm) -------------- Packing ----* (Please read the precautions on the back page first.) Printed by the cooperative 520274 A7 B7______ Five. Explanation of splash month (21) Aphid, white-backed planthopper, orange aphid, wheat whitefly, greenhouse whitefly, and grape nodule aphid; • termites (Isooptera) such as Calotermes flavicollis, Leucotermes flavipes, Reticulitermes lucifugus, and Termes natalensis; • Orthopterans such as European salamanders, Tibetan flying gifts, double-banded grasshoppers, red-legged grasshoppers, Mexican grasshoppers, migratory grasshoppers, Rocky Mountain grasshoppers, red-winged locusts, American grasshoppers Mighty, Schistocerca peregrina, Stauronotus maroccanus, Badlands grasshopper, and domestic crickets, Oriental crickets, German cockroaches, and American cockles Insects, Brevipalpus phoeni cis, alfalfa moss madder, hellebore oriental leaf snail, Texas orange leaf worm Yu, Eriophyes sheldoni, grass small snail, apple red for spider, orange whole snail, orange rust snail, multi-eating Selenium elegans, Vermilion leaf snail, Tetranychus kanzawai, Pacific red leaf snail, Nematode Yu, beak monuments such as American flower ticks, Amblyomma variegatum, Persian hidden horn monument, square-headed tick, Boophilus decoloratus, tiny tick loss, Dermacentor silvarum , Hyalomma truncatum, Ixodes sheep, Ixodes rubicundus, Ornithodorus moubata, ear tick residual taste, Rhipicephalus appendiculatus, Rhipicephalus evertsi, Sarcoptes scabiei, Tetranychus cinnabarinus, Tetranychus kanzawai, Tetranychus pacificus, Tetranychus telarius and Tetanychus urticae; • Meloidogyne Nematoda e.g. For example, horse # root nematodes, peanut root-knot nematodes and cotton root nematodes, forming cyst nematodes such as Globodera rostochiensis, -24- This paper size applies the Chinese National Standard (CNS) A4 specification (210 X 297 mm) ----- --------- Installation——--(Please read the precautions on the back page first ) Order · • Line-520274 A7 B7 Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

五、發明說明(22) Heterodera avenae、大豆線蟲及 Heterodera schachtii、 Heterodera trifolii 莖及葉線蟲如 Belonolaimus longicaudatus、破壞性莖線蟲、玉米莖線蟲、 Heliocotylenchus multicinctus、Longidorus elongatus、 Radopholus similis、Rotylenchus robustus、Trichodorus primitivus、Tylenchorhynchus claytoni、Tylenchorhynchus dubius、Pratylenchus neglectus、Pratylenchus penetrans、 Pratylenchus curvitatus N Pratylenchus goodeyi 0 在農地條件下,控制動物害蟲活性成份之施用率通常爲 0.01至2.0,較佳爲0.02至1.0公斤/公頃。 本發明之混合物特別適用控制稻之植物疾病與有害昆蟲。 化合物I與至少一種化合物11至XI之混合物可一起或分別 同時施用或循序施用,於分別施用時,順序通常對控制結 果無任何影響。 視所需效果種類而定,本發明混合物之施用率(尤其是農 業作物)自0.01至8公斤/公頃,較好0.1至5公斤/公頃,尤其 是0.5至3.0公斤/公頃。 化合物I之施用率爲0·01至2.5公斤/公頃,較好0.05至2.5公 斤/公頃,尤其是0.1至1·〇公斤/公頃。 對種子處理而言,混合物之施用率通常自0.001-至250克/ 公斤種子,較好0.01至1〇〇克/公斤,尤其是〇.〇1至50克/公 若欲防治植物致病性有害眞菌一,則化合物I及至少一種11 至XI之分別或一起施用,或含化合物I及至少一種化合物II -25- 本紙張尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) (請先閱讀背面之注意事項 本頁) 裝 訂: 丨線· 520274 王入K混合物可 A7 五、發明說明(23 ) 植物或植物播種前或後之土 或、或植物萌發前或後,噴霧或撒粉而進行。 本發明之殺眞菌協同混合物可調配成立即喷霧之溶液、箱 末及懸浮液態或調配成高度濃縮水性、油性或其他縣^ =、分散液、乳液、油分散液、糊劑、粉劑、供散播之私 貝或顆粒態,並藉噴霧、霧化、撒粉、散播或撒水施用; ,用狀態視所欲目的而異;任何例中,須儘可能確使本韻 明混合物分佈細密及均勻。 •該調配物係依已知方式製備,例如以溶劑及/或載體及若 需要則使用乳化劑及分散劑稀釋該活性成分,若使用水作 爲稀釋劑則亦可使用其他溶劑作爲輔助溶劑。此目的之適 宜輔助齊:基:上如下:溶劑如芳族(如二甲苯)、氣化芳族 (口乳年)、鏈;^(礪油館份)、醇類(如甲醇、丁醇)、酮類 (如環己嗣)、胺類(如乙醇胺、二甲基甲醯胺)及水;載劑如 物(如高嶺土、黏土、滑石、白堊)及研磨合成 如細粒氧切、沙酸鹽);乳化劑如非離子性及陰離 =化劑(如川埽脂肪醇酿、燒續酸酿及芳磺酸醋) 及为政劑如木質亞硫酸鹽廢液及甲基纖維素。 適宜(界面活性劑爲芳族續酸如木質_、酉分.、文及二丁 ;菩=驗金屬鹽、驗土金屬鹽及铵鹽,脂肪酸、貌 二?元方基磺酸之鹼金屬鹽、鹼土金屬鹽及銨鹽,垸基 =及脂!醇硫酸鹽’及硫酸化十己-、十七-及十八燒 义现,或脂肪醇二醇醚之鹽Γ績酸化茶及其衍生物斑甲 κ縮合物、茶或茶續酸與紛及甲路之縮合物,聚氧乙缔 i_______ - 26 -V. Description of the invention (22) Heterodera avenae, soybean nematodes and Heterodera schachtii, Heterodera trifolii stems and leaf nematodes such as Belonolaimus longicaudatus, destructive stem nematodes, corn stem nematodes, Heliocotylenchus multicinctus, Longidorus elongatus, Radopholus similius, RotylenTrusus, Rotylen Tylenchorhynchus claytoni, Tylenchorhynchus dubius, Pratylenchus neglectus, Pratylenchus penetrans, Pratylenchus curvitatus N Pratylenchus goodeyi 0 In agricultural conditions, the application rate of active ingredients for controlling animal pests is usually 0.01 to 2.0, preferably 0.02 to 1.0 kg / ha. The mixture of the invention is particularly suitable for controlling plant diseases and harmful insects in rice. The mixture of Compound I and at least one of Compounds 11 to XI can be applied together or separately or simultaneously or sequentially. When applied separately, the order usually does not have any effect on the control results. Depending on the type of effect desired, the application rate of the mixture of the invention (especially for agricultural crops) is from 0.01 to 8 kg / ha, preferably from 0.1 to 5 kg / ha, especially from 0.5 to 3.0 kg / ha. The application rate of Compound I is from 0.01 to 2.5 kg / ha, preferably from 0.05 to 2.5 kg / ha, especially from 0.1 to 1.0 kg / ha. For seed treatment, the application rate of the mixture is usually from 0.001 to 250 g / kg of seed, preferably from 0.01 to 100 g / kg, and especially from 0.01 to 50 g / kg. Harmful fungi I, compound I and at least one of 11 to XI are applied separately or together, or contain compound I and at least one compound II -25- This paper size applies to China National Standard (CNS) A4 (210 X 297 mm) ) (Please read the precautions on the back page first) Binding: 丨 line · 520274 King into K mixture can A7 V. Description of the invention (23) Plant or soil before or after sowing, or spray before or after germination, spray Or dusting. The fungicidal synergistic mixture of the present invention can be formulated into a solution, an end of a tank and a suspended liquid for immediate spraying or a highly concentrated aqueous, oily or other county ^, a dispersion, an emulsion, an oil dispersion, a paste, a powder, Private shells or granules for dissemination, and application by spraying, atomizing, dusting, dispersing or watering; the state of use varies according to the intended purpose; in any case, the distribution of this rhyme mixture must be as fine as possible and Even. • The formulation is prepared in a known manner, such as diluting the active ingredient with a solvent and / or carrier and, if necessary, emulsifiers and dispersants. If water is used as a diluent, other solvents may be used as auxiliary solvents. Suitable assistants for this purpose are as follows: base: the following: solvents such as aromatics (such as xylene), gasification aromatics (oral milk year), chains; ^ (dark oil museum), alcohols (such as methanol, butanol ), Ketones (such as cyclohexane), amines (such as ethanolamine, dimethylformamide) and water; carriers such as substances (such as kaolin, clay, talc, chalk) and grinding synthesis such as fine-grained oxygen cutting, Saline salt); emulsifiers such as non-ionic and anionic = chemical agents (such as Chuanxiong fatty alcohol brewing, burning acid brewing and aromatic sulfonic acid vinegar) and political agents such as lignosulfite waste liquor and methyl fiber Vegetarian. Suitable (Surface active agent is aromatic continuous acid such as wood _, 酉., Wen and dibutyl; pu = metal test salt, soil test metal salt and ammonium salt, fatty acid, appearance two? Yuan square sulfonic acid alkali metal Salt, alkaline earth metal salt and ammonium salt, fluorenyl group = and fat! Alcohol sulfate 'and sulfated ten-hexyl-, seventeen- and eighteen-yakiri, or fatty alcohol glycol ether salts Derivatives Condensate κ, condensate of tea or tea acid, and polycondensation, polyoxyethylene i_______-26-

本紙張尺度適財國國規格(210 XThis paper is suitable for the country's specifications (210 X

520274 五、發明說明(24 ) 辛基酚醚、乙氧化異辛基_、辛 一 肀基或壬基-酚、烷基酚聚二 醇醚、三丁基苯基聚二醇醚 ^ ^ 砭万基聚醚醇、異十三煩 醇、脂肪·醇、環氧乙烷縮合物、 广 r # 0TJ, π 乳化毘麻油、聚氧乙歸 坑基醚或聚氧丙烯烷基醚、月 1径知禾一醇醚乙酸酯、山梨 糖醇、木質亞硫酸廢液或甲基纖維素。 粉末、供散播之物質及粉劑可藉混合或一起研磨化合物】 及至少一種化合物π·或化合物及至少一種化合物Η XI之混合物,與固體載體而製備。 、顆粒劑(如包衣顆粒、浸潤顆粒或均質顆粒卜般係使活性 成分(或諸活性成分)結合至固體载體上而製備。 填料或固體載體爲例如礦土氧化矽、矽膠、矽酸鹽、滑 石、高嶺土、石灰石、石灰、白堊、紅玄武土、黃土、黏 土、白雲石、矽藻土、硫酸鈣、硫酸鎂、氧化鎂、研磨合 成材料及肥料如硫酸銨、磷酸銨、硝酸銨、尿素、及植物 來源之產物如穀粉、樹皮粉、木粉及堅果穀粉、纖維素粉 末或其他固體載體。 此凋配物通常包括自〇 · 1至9 5重量%,較好〇 · 5至9 〇重量〇/0 之任一化合物I及至少一種化合物Ζ Ζ至X j或化合物I與至少 種11至X I之混合物。活性成分使用純度自9〇%至1 〇〇%, 較好95%至100%者(依NMR光譜或HPLC測定)。 - 化合物I及至少一種化合物IISXI,混合物或對應調配物 可以殺興菌有效量之混合物或殺眞菌有效量之化合物I及至 少一種化合物11至XI化合物(分別施用之例中)處理有害眞 菌、其棲息處、或欲防治眞菌之植物、種子、土壤、區 27 本紙尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) 裝--- -. (請先閱讀背面之注意事項寫本頁) 訂· ί線· 經濟部智慧財產局員工消費合作社印製 520274 A7 B7 五、發明說明(25 域、材料或空間免受侵害。 施用可在受有害眞菌感染前後進行。 此種包括活性成分之製劑實例爲: I·含90重量份活性成分及10重量份N-甲基吡咯烷酮之溶 液;此溶液宜以微滴劑使用; ' II·含20重量份活性成分、80重量份二甲基、1〇重量份之 8至10莫耳環氧乙烷與}莫耳油酸^單乙醇醯胺之加成 物、5重量份十二fe基苯續酸躬鹽、5重量份之莫耳 ¥氧乙烷與1莫耳蓖麻油之加成物之混合物;藉使此溶 液微細分佈於水中獲得分散液; III·含20重量份活性成分、4〇重量份環己酮、3〇重量份異 丁醇、20重量份之40莫耳環氧乙烷與1莫耳蓖麻油之加 成物之水性分散液; IV·含20重量份活性成分、25重量份環己醇、65重量份滞 點210 土 280C之礦油館份及1〇重量份之4q莫耳環氧乙 與1莫耳蓖麻油之加成物之水性分散液; V.於錘磨機中研磨之含80重量份活性成分、3重量份二異 丁基莕-1-磺酸鈉鹽、10重量份得自亞硫酸鹽廢液之木 質磺酸鈉鹽及7重量份粉碎矽膠之混合物;藉微細分佈 該混合物於水中獲得噴霧混合物; - VI · 3重量份活性成分及9 7重量份細粒高嶺土之緊密混合 物;此粉塵包括3重量%活性成分; VII. 3 0重量活性成分、9 2重量#粉碎矽膠及8重量份已噴霧 至此石夕膠表面之石犧油之緊密混合物;此調配物賦與活 -28- 本紙?長尺度適用中國國家標準(CNS)A4規格(210 x 297公釐) 7 , 裝— (請先閱讀背面之注意事項本頁) 訂· ;線. 經濟部智慧財產局員工消費合作社印製 520274 A7 _ B7___ 五、發明說明(27 ) X當使用濃度a之活性成分a時,以未處理對照組之%表示 之效率 y當使用濃度b之活性成分B時,以未處理對照組之%表示 之效率 使用貫例1 ··對抗稻瘟菌之活性(保護) 用活性成份之水性製劑噴灑盆栽稻苗,,台農67 ”之葉片至 /土合合爲止,綰製劑係由含丨0 %活性成份,6 3 %環己酮及 27 /〇礼化劑之貯液所製備。次日,用稻痕菌之水性孢子懸浮 劑接種植物。接著將受試植物置於22_2^c&95_99%相對溼 度之溫室6天。然後目測葉片感染之進展程度。 殳感木葉面積百分比之目視測定値以對未處理對照組之百 分比表7F轉化成效率。效率〇表示如未處理對照組相同之疾 病程度,效率1〇〇表不〇%疾病。使用柯比程式((^丨0,3上· "Calculating synergistic and antagonistic responses of herbicide Combinations”,Weeds,15,第 2(K22 頁,i967)測定 活性成分組合物之預期效率並與觀察效率比較。 所用化合物Γ爲下列成分a): 實驗結果見於下表1及2 : _______30_ 本紙?長尺度適用中國國家標準(CNS)A4規格(210 X 297公釐) --------------裝—— * # (請先閱讀背面之注意事項本頁) 訂: 經濟部智慧財產局員工消費合作社印製520274 V. Description of the invention (24) Octylphenol ether, ethoxy isooctyl_, octanyl or nonyl-phenol, alkylphenol polyglycol ether, tributylphenyl polyglycol ether ^ ^ 砭Wanji Polyether Alcohol, Isotridecyl Alcohol, Fatty Alcohol, Ethylene Oxide Condensate, Cantonal R # 0TJ, π Emulsified Vima Oil, Polyoxyethylene Benzyl Ether or Polyoxypropylene Alkyl Ether, Month 1 It is known that glutarol ether acetate, sorbitol, lignosulfite waste liquid or methyl cellulose. Powders, substances for dispersal and powders can be prepared by mixing or grinding together a compound] and a mixture of at least one compound π · or a compound and at least one compound Η XI with a solid carrier. Granules (such as coated granules, infiltrated granules, or homogeneous granules) are prepared by combining the active ingredient (or active ingredients) on a solid support. The filler or solid support is, for example, mineral silica, silica gel, silicic acid Salt, talc, kaolin, limestone, lime, chalk, red basalt, loess, clay, dolomite, diatomaceous earth, calcium sulfate, magnesium sulfate, magnesium oxide, abrasive synthetic materials and fertilizers such as ammonium sulfate, ammonium phosphate, ammonium nitrate , Urea, and plant-derived products such as cereal flour, bark flour, wood flour and nut cereal flour, cellulose powder or other solid carriers. This wither usually comprises from 0.1 to 95% by weight, preferably 0.5 to 90 weight 0/0 of any one of compound I and at least one compound Z Z to X j or a mixture of compound I and at least 11 to XI. The active ingredient is used in a purity of 90% to 100%, preferably 95%. Up to 100% (determined by NMR spectrum or HPLC)-Compound I and at least one compound IISXI, the mixture or the corresponding formulation can kill a mixture of fungicidal effective amount or fungicidal effective amount of compound I and at least one Compounds 11 to XI (in the case of separate application) are used to treat harmful fungi, their habitats, or plants, seeds, soil, and areas where fungi are to be controlled. 27 Paper size applies to Chinese National Standard (CNS) A4 (210 X 297) (Mm) Packing ----. (Please read the notes on the back to write this page) Order · Printed by the Intellectual Property Bureau of the Ministry of Economic Affairs, printed by the Consumer Cooperative 520274 A7 B7 V. Description of the invention (25 domains, materials or space Protect from damage. Application can be performed before and after being infected by harmful fungi. Examples of such preparations including active ingredients are: I. A solution containing 90 parts by weight of the active ingredient and 10 parts by weight of N-methylpyrrolidone; Use of drops; II. Contains 20 parts by weight of active ingredient, 80 parts by weight of dimethyl, 10 parts by weight of 8 to 10 moles of ethylene oxide and mololeic acid ^ monoethanolamine, A mixture of 5 parts by weight of dodecaphenoxybenzoic acid salt, 5 parts by weight of an adduct of mol ¥ oxyethane and 1 mol castor oil; the solution is finely distributed in water to obtain a dispersion; III · Contains 20 parts by weight of active ingredient, 40 parts by weight of cyclohexanone, 30%. Aqueous dispersion of adduct of 20 parts by weight of isobutanol, 20 parts by weight of 40 moles of ethylene oxide and 1 mole of castor oil; IV. 20 parts by weight of active ingredient, 25 parts by weight of cyclohexanol, 65 parts by weight Stagnation point 210 to 280C, mineral oil, and 10 parts by weight of 4q mole of ethylene oxide and 1 mole of castor oil adduct of the aqueous dispersion; V. 80 mill parts by weight in a hammer mill A mixture of ingredients, 3 parts by weight of diisobutylphosphonium-1-sulfonate sodium salt, 10 parts by weight of lignosulfonic acid sodium salt obtained from sulfite waste liquid, and 7 parts by weight of crushed silicone; finely distribute the mixture in water Obtaining a spray mixture;-VI. An intimate mixture of 3 parts by weight of the active ingredient and 97 parts by weight of fine-grained kaolin; this dust includes 3% by weight of the active ingredient; VII. 30% by weight of the active ingredient, 9 2% by weight of crushed silicone and 8% by weight An intimate mixture of stone sacrificial oil that has been sprayed onto the surface of this stone glue; this formulation gives live -28- this paper? Long-scale applicable to China National Standard (CNS) A4 specifications (210 x 297 mm) 7, Packing-( Please read the caution page on the back first) Order ·; Line. Ministry of Economic Affairs Intellectual Property Printed by the Bureau ’s Consumer Cooperative 520274 A7 _ B7___ V. Description of the invention (27) X When using active ingredient a at concentration a, the efficiency expressed as% of untreated control group y When using active ingredient B at concentration b, use The efficiency indicated by the% of the untreated control group. Example 1 · Activity against rice blast fungus (protection) Spray the potted rice seedlings with an aqueous preparation of the active ingredient, and the leaves of Tainong 67 "until the soil is combined, the 绾 preparation It is prepared from a stock solution containing 0% active ingredients, 63% cyclohexanone, and a 27/0 chemotherapeutic agent. The next day, the plants were inoculated with an aqueous spore suspension of the rice fungus. The test plants were then placed in a greenhouse at 22_2c & 95_99% relative humidity for 6 days. Then visually inspect the progress of leaf infection. Visual determination of the percentage of woody leaf area of the sensation. Table 7F was converted to efficiency as a percentage to the untreated control group. An efficiency of 0 indicates the same degree of disease as the untreated control group, and an efficiency of 100 indicates 0% of the disease. Using the Kirby formula ((^ 丨 0, 3 on " Calculating synergistic and antagonistic responses of herbicide Combinations ", Weeds, 15, page 2 (K22, i967) to determine the expected efficiency of the active ingredient composition and compare it with the observed efficiency The compound Γ used is the following component a): The experimental results are shown in the following Tables 1 and 2: _______30_ This paper? The long scale applies the Chinese National Standard (CNS) A4 specification (210 X 297 mm) ---------- ---- 装 —— * # (Please read the note on the back page first) Order: Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs

520274 A7 B7 五、發明說明(28 ) 表1 Ex. 活性成分 濃度呈ppm 未處理對照組 之%功效 1C 無 (100%疾病) 0 2C 化合物Γ 2.0 20 0.5 0 3C 化合物11 2.0 0 0.5 0 4C 化合物V 2.0 0 0.5 0 表2 : E X. 本發明之混合物(濃度 至 ppm) 觀察功效 計算功效* 5 2 ppm Γ + 2 ppm II 50% 20% 6 0.5 ppm Γ + 0.5 ppm II 30% 10% 7 2 ppm Γ + 2 ppm V 40% 20% 8 0.5 ppm Γ+0.5 ppm V 25% 10% *)使用柯比程式計算者。 貫驗結果顯示所有混合比例之觀察功效均比使用柯比程式 计舁之效率高。 - --------------裝--- f S (請先閱讀背面之注音?事項本頁) 訂 •線. 經濟部智慧財產局員工消費合作社印製 格 規 A4 S) N (C 準 標 家 國 國 用 IX. 7 个 -31 - 釐 公 7 9 2 X ο 520274 第88104751號專利申請案 中文說明書修正頁(90年3月)五、發明説明(5 ) L 與 b)至少一種選自式II至XI之殺昆蟲劑520274 A7 B7 V. Description of the invention (28) Table 1 Ex. Active ingredient concentration in ppm Untreated control group% efficacy 1C None (100% disease) 0 2C compound Γ 2.0 20 0.5 0 3C compound 11 2.0 0 0.5 0 4C compound V 2.0 0 0.5 0 Table 2: E X. The mixture of the present invention (concentration to ppm) Calculate the efficacy by observing the efficacy * 5 2 ppm Γ + 2 ppm II 50% 20% 6 0.5 ppm Γ + 0.5 ppm II 30% 10% 7 2 ppm Γ + 2 ppm V 40% 20% 8 0.5 ppm Γ + 0.5 ppm V 25% 10% *) Calculated using Kirby formula. The test results show that the observed power of all mixed ratios is more efficient than that calculated using the Kirby program. --------------- Installation --- f S (Please read the phonetic on the back? Matters page) Order • Thread. The Intellectual Property Bureau, Ministry of Economic Affairs, Consumer Consumption Cooperatives prints the code A4 S) N (C quasi-standard countries IX. 7 -31-centimeters 7 9 2 X ο 520274 Patent Application No. 88104751 Patent Specification Revised Page (March 90) V. Description of Invention (5) L And b) at least one insecticide selected from Formulae II to XI

ch3nh (III; (IV) (請先閲讀背面之注意事項再填寫本頁) 訂 經濟部中央標準局員工消費合作社印製ch3nh (III; (IV) (Please read the notes on the back before filling out this page) Order Printed by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs

ClCl

NN

Cl NHCl NH

CN (V) 2 CF,CN (V) 2 CF,

OCONHCHOCONHCH

(VI) -8- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 520274 第088104751號專利申請案 中文說明書修正頁(91年11月γ Α7 Β7 91. 11. 29 五、發明説明( a ch3 I 3(VI) -8- This paper size applies Chinese National Standard (CNS) A4 specification (210X297 mm) 520274 No. 088104751 Patent Application Chinese Specification Correction Page (November 91 γ Α7 Β7 91. 11. 29 V. Invention Description (a ch3 I 3

(VII) OCON—S — N[(CH2)3CH3]s -〇v CH,(VII) OCON—S — N [(CH2) 3CH3] s -〇v CH,

本紙張尺度適用中國國家標準(CNS) A4規格(210 X 297公釐)This paper size applies to China National Standard (CNS) A4 (210 X 297 mm)

經濟部中央標準局員工消費合作社印製 520274 第88104751號專利申請案 中文說明書修正頁(90年$月) 五、發明説明(7 本發明之一項目的係提供具良好殺真菌活性之混合物, 尤其係對抗稻米之真菌疾病,另一方面係提供良好殺昆蟲 活性。由於培養稻米之氣候區,亦常遇到許多有害昆蟲, 故期望殺真菌性與殺昆蟲活性之組合。 吾等發現該標的可以申請專利範圍第1項所請之混合物達 成。 式I化合物係本身已知的且見述於文獻(WO 97/15,552)。 式II至VII之殺昆蟲劑亦為已知的且見述於文獻。此外, 彼等可視需要依下述括弧中所述商品名市售獲得: II : EP-A 192,060,俗名:imidacloprid(商品名:Admire®,Printed by the Consumer Standards Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 520274 No. 88104751 Patent Application Chinese Specification Revised Page (90 / month) V. Description of the Invention (7 One of the items of the invention is to provide a mixture with good fungicidal activity, especially It is an antifungal disease against rice, and on the other hand, it provides good insecticidal activity. Since the climatic zone in which rice is cultivated often encounters many harmful insects, a combination of fungicidal and insecticidal activity is expected. We found that the target can The mixture requested by the scope of the patent application is achieved in item 1. The compounds of formula I are known per se and are described in the literature (WO 97 / 15,552). Insecticides of the formulae II to VII are also known and described in the literature In addition, they are commercially available under the trade names described in the following brackets as required: II: EP-A 192,060, common name: imidacloprid (trade name: Admire®,

Gaucho⑧,來自 Bayer); III :俗名:acetamiprid(商品名:Mospilan@,來自 NipponGaucho⑧, from Bayer); III: Common name: acetamiprid (trade name: Mospilan @, from Nippon

Soda); IV · CAS RN 120738-89-8,商品名:nitenpyram(商品名:Soda); IV · CAS RN 120738-89-8, trade name: nitenpyram (trade name:

Bestgard⑧,來自 Takeda Chemicals); V : Colliot等人·,proc. Br· Conf· Dis· JL,(1992),29,俗名: fipronil(商品名:Regent⑧,來自 Rhone-Poulenc); VI : US 3,474,170; US 3,474,171 及DE-C 1,493,646 ;俗名: carbofuran(商品名:Curaterr®,來自 Bayer; Furadan®,來 自 FMC); VII: Proc· ΒΓ· Crop Prot. Conf· 2 (1979),557,俗名: cairbosulfan(商品名:Marshall®,來自 FMC); VIII : FR-A 2,489,329; Proc. Int. Congr. Plant Port. 10th5 2_ (1983),360,俗名:benfuracarb(商品名:Oncol ⑧,來自 -10 - 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) (請先閲讀背面之注意事項再填寫本頁)Bestgard (R) from Takeda Chemicals); V: Colliot et al., Proc. Br · Conf · Dis · JL, (1992), 29, common name: fipronil (trade name: Regent (R) from Rhone-Poulenc); VI: US 3,474, 170; US 3,474,171 and DE-C 1,493,646; common name: carbofuran (trade name: Curaterr® from Bayer; Furadan® from FMC); VII: Proc · ΒΓ · Crop Prot. Conf · 2 (1979), 557, common name: cairbosulfan (trade name: Marshall®, from FMC); VIII: FR-A 2,489,329; Proc. Int. Congr. Plant Port. 10th5 2_ (1983), 360, common name: benfuracarb (trade name: Oncol ⑧, From -10-This paper size applies Chinese National Standard (CNS) A4 (210X 297mm) (Please read the precautions on the back before filling this page)

520274 第088HH751號專利申請案 中文說明書修正頁(91年11月) A7 五、發明説明(26 ) 公告衣|繁O:g— V·丨丨 ί __,丨__ Ν__ι__·_ — _ι_ι· .,_ ___ , -一 性成分良好黏著性; VIII. 4 0重量活性成分、丨〇重量份酚磺酸/脲/甲醛縮合物之 鈉鹽、2重量份矽膠及48重量份水之安定水性分散液; 此分散液可再經稀釋; IX· 20重量活性成分、2重量份十二烷基苯磺酸鈣鹽、8重 量份脂肪醇聚二醇醚、2 0重量份酚磺酸/脲/甲醛縮合 物之鈉鹽及8 8重量份石堪礦油之安定油性分散液。 本發明之混合物之協同活性依據下列實驗證明: 活性成分(分別或一起)調配成於含6 3重量%環己酮及2 7 重量%乳化劑之混合物中之1 〇 %乳液,並以水稀釋至所需 度。 藉測定受感染葉片面積百分比進行評估。該等百分比轉 化成效率。效率(里J使用亞伯特氏(Abb〇t,s)方程式如下計 算: W=(l-a//5) · 1〇〇 α相當於經處理植物受真菌感染之%,及 /5相當於未處理植物受真菌感染之。/〇。 效率0表示經處理植物受感染程度相當於未處理之對辟組 植物;效率100表示經處理植物未受感染。 使用柯比(Colbyfs)方程式[R.s· Colby, Weeds U,20-22 (1 967)]測定活性成分混合物之預期效率並與所觀察之效率 比較。 柯比程式:E = x + y-x · y/l 〇〇 E當使用濃度a及b之活性成分A及B之混合物時,以未處理 對照組之%表示之預期效率 -29- 本紙張尺度適用中國國家標準(CNS) A4規格(210 X 297公釐) *-----520274 Patent Application No. 088HH751 Revised Chinese Manual (November 91) A7 V. Description of Invention (26) Bulletin | 繁 O: g— V · 丨 丨 ί __, 丨 __ Ν__ι__ · _ — _ι_ι ·. , _ ___,-Good adhesion of unisex ingredients; VIII. 40 weight active ingredient, 〇〇part by weight sodium salt of phenolsulfonic acid / urea / formaldehyde condensate, 2 parts by weight of silicone and 48 parts by weight of stable aqueous dispersion This dispersion can be further diluted; IX. 20 weight active ingredient, 2 parts by weight calcium dodecylbenzenesulfonate, 8 parts by weight fatty alcohol polyglycol ether, 20 parts by weight phenolsulfonic acid / urea / Sodium salt of formaldehyde condensate and stable oily dispersion of 88 parts by weight of shikan mineral oil. The synergistic activity of the mixture of the present invention is proved by the following experiments: The active ingredients (respectively or together) are formulated into a 10% emulsion in a mixture containing 63% by weight of cyclohexanone and 27% by weight of an emulsifier, and diluted with water. To the required degree. Estimated by measuring the percentage of infected leaf area. These percentages translate into efficiency. Efficiency (where J is calculated using the Abbot's, S) equation as follows: W = (la // 5) · 100α is equivalent to the% of the treated plant infected with the fungus, and / 5 is equivalent to the untreated Treated plants are infected by fungi. / 0. Efficiency 0 means that the treated plants are infected to the same extent as the untreated counterparts; efficiency 100 means that the treated plants are not infected. Using the Colbyfs equation [Rs · Colby , Weeds U, 20-22 (1 967)] Determine the expected efficiency of the active ingredient mixture and compare it with the observed efficiency. Kirby formula: E = x + yx · y / l 〇〇E When using concentrations a and b For mixtures of active ingredients A and B, the expected efficiency expressed as% of the untreated control group -29- This paper size applies the Chinese National Standard (CNS) A4 specification (210 X 297 mm) * -----

Claims (1)

520274 第088104751號專利申請案 A8 B8 中文申請專利範圍修正本(9 Γ年 T1"月 了一·^~1 91 11. ; r 六、申請專利範圍 公告本 1.^— 'Μ -14 一種作物保護之混合物,包括呈協同有效量之下列成分 作為活性成份 a)式(I)之苯乙酸衍生物 R3520274 Patent Application No. 088104751 A8 B8 Chinese Patent Application Scope Amendment (9 Γ Year T1 " Month · ^ ~ 1 91 11.) r Six. Patent Application Announcement 1. ^ — 'Μ -14 A crop Protected mixture comprising, in synergistically effective amounts, the following ingredients as active ingredient a) phenylacetic acid derivative R3 of formula (I) (工)' 其中取代基及參數具有下列定義: X 係 noch3; Y 係 NR ; R1 'R 分別獨立為氫或CrC4-烷基; R3 係氫或Ci-CV烷基; R4、R6 分別獨立為氫或crc4-烷基; R5 係氫或CrC4-烷基; 及其鹽, 與 b)至少一種式(II)、(V)、(X)及(XI)之化合物(工) 'Wherein the substituents and parameters have the following definitions: X is noch3; Y is NR; R1' R is independently hydrogen or CrC4-alkyl; R3 is hydrogen or Ci-CV alkyl; R4 and R6 are each independently Hydrogen or crc4-alkyl; R5 is hydrogen or CrC4-alkyl; and salts thereof, and b) at least one compound of formula (II), (V), (X), and (XI) 520274 A8 B8 C8 D8520274 A8 B8 C8 D8 Cl (\ • N 2 ·根據申請專利範圍第1項之混合物,係調整成兩部份, 其中一部份包括於固體或液體載體中之化合物(1),而另 一部份包拾於固體或液體載體中至少一種化合物(ιι)、 (v)、(X)及(χυ。 3 · —種防治有害真菌之方法,包括以根據申請專利範圍第 1或2項之混合物處理真菌,其棲息處,或欲防治真菌免 受其侵¥之材料、植物、種子、土壤、區域或空間,其 中化合物(I)及至少一種化合物(11)、(V)、(χ)及(χι) 可同時、一起或分別或依序施用。 4.根據申請專利範圍第3項之方法,其中有害真菌,其樓 -2 - 520274 8 8 8 8 A B c D 六、申請專利範圍 息處,或欲防治真菌免受其侵害之材料、植物、種子、 土壤、區域或空間係用0.005至1公斤/公頃之根據申請專 利範圍第1項中化合物(I)處理。 -3- 本紙張尺度適用中國國家標準(CNS) A4規格(210 X 297公釐)Cl (\ • N 2 · The mixture according to item 1 of the scope of the patent application is adjusted into two parts, one part of which contains the compound (1) in a solid or liquid carrier, and the other part of which is packed in a solid Or at least one compound (ιι), (v), (X) and (χυ.) In a liquid carrier 3. A method for controlling harmful fungi, comprising treating the fungus with a mixture according to item 1 or 2 of the scope of the patent application and inhabiting it Or materials, plants, seeds, soil, areas or spaces where fungi are to be protected from invasion, where compound (I) and at least one compound (11), (V), (χ) and (χι) may be simultaneously , Together or separately or sequentially. 4. The method according to item 3 of the scope of the patent application, in which harmful fungi, its floor-2-520274 8 8 8 8 AB c D 6. The area of the patent application, or fungal control Materials, plants, seeds, soil, areas or spaces protected from them are treated with 0.005 to 1 kg / ha according to the compound (I) in item 1 of the scope of the patent application. -3- This paper scale applies Chinese national standards ( CNS) A4 size (210 X 297 PCT)
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