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CA2311490A1 - Technologie en phase solide pour l'elaboration de bibliotheques combinatoires par via ancrage par liaison amide - Google Patents

Technologie en phase solide pour l'elaboration de bibliotheques combinatoires par via ancrage par liaison amide Download PDF

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Publication number
CA2311490A1
CA2311490A1 CA002311490A CA2311490A CA2311490A1 CA 2311490 A1 CA2311490 A1 CA 2311490A1 CA 002311490 A CA002311490 A CA 002311490A CA 2311490 A CA2311490 A CA 2311490A CA 2311490 A1 CA2311490 A1 CA 2311490A1
Authority
CA
Canada
Prior art keywords
compounds
resin
scheme
general formula
linker
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA002311490A
Other languages
English (en)
Inventor
Tony Johnson
Martin Quibell
Joanne Howe
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Medivir UK Ltd
Original Assignee
Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB9724853.8A external-priority patent/GB9724853D0/en
Priority claimed from GBGB9808744.8A external-priority patent/GB9808744D0/en
Application filed by Individual filed Critical Individual
Publication of CA2311490A1 publication Critical patent/CA2311490A1/fr
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/04—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length on carriers
    • C07K1/047—Simultaneous synthesis of different peptide species; Peptide libraries
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/74—Unsaturated compounds containing —CHO groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/04—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length on carriers
    • C07K1/042—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length on carriers characterised by the nature of the carrier
    • C—CHEMISTRY; METALLURGY
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B40/00—Libraries per se, e.g. arrays, mixtures
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Analytical Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Other Resins Obtained By Reactions Not Involving Carbon-To-Carbon Unsaturated Bonds (AREA)

Abstract

L'invention concerne une technique permettant d'éliminer l'épimérisation de l'acide aminé terminal C.alpha. dans une séquence peptidique protégée, durant le couplage, en utilisant la fraction de protection représentée en (1), que l'on appelle "lieur précurseur". Cette fraction a un certain nombre de caractéristiques. Ainsi, le groupe fonctionnel R et la fonction 2-hydroxyle sont en position para l'un vis-à-vis de l'autre, et le résidu éther est en position para vis-à-vis du résidu aldéhyde. R1 est un groupe alkyle donneur d'électrons. Le groupe R est une fraction capable de passer facilement d'un rôle de retrait d'électrons à un rôle donneur d'électrons et vice versa. Cela repose sur la notion de mécanisme de sécurité. Le principe selon lequel une liaison stable passe aisément à l'état de liaison instable en un point approprié durant une synthèse a été appliqué à la chimie des peptides pour l'élaboration de lieurs et de groupes de protection. Une approche a consisté à exploiter la facilité de conversion réductrice d'un sulfoxyde en sulfure. Lorsqu'elle est appliquée au lieur précurseur (1), cette approche permet d'obtenir des fractions de protection fonctionnelles appelées "composés lieurs".
CA002311490A 1997-11-26 1998-11-26 Technologie en phase solide pour l'elaboration de bibliotheques combinatoires par via ancrage par liaison amide Abandoned CA2311490A1 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GBGB9724853.8A GB9724853D0 (en) 1997-11-26 1997-11-26 A solid-phase technology for the preparation of combinatorial libraries through amide-bond anchoring
GB9808744.8 1998-04-25
GBGB9808744.8A GB9808744D0 (en) 1998-04-25 1998-04-25 A solid-phase technology for the preparation of combinatorial libraries through amide-bond anchoring
GB9724853.8 1998-04-25
PCT/GB1998/003523 WO1999026902A1 (fr) 1997-11-26 1998-11-26 Technologie en phase solide pour l'elaboration de bibliotheques combinatoires par via ancrage par liaison amide

Publications (1)

Publication Number Publication Date
CA2311490A1 true CA2311490A1 (fr) 1999-06-03

Family

ID=26312654

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002311490A Abandoned CA2311490A1 (fr) 1997-11-26 1998-11-26 Technologie en phase solide pour l'elaboration de bibliotheques combinatoires par via ancrage par liaison amide

Country Status (5)

Country Link
EP (1) EP1034154A1 (fr)
JP (1) JP2001524457A (fr)
AU (1) AU734992B2 (fr)
CA (1) CA2311490A1 (fr)
WO (1) WO1999026902A1 (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AUPP616598A0 (en) 1998-09-25 1998-10-15 University Of Queensland, The Auxiliary for amide bond formation
AUPP616498A0 (en) 1998-09-25 1998-10-15 University Of Queensland, The Synthesis of cyclic peptides
CN117924235B (zh) * 2024-01-19 2024-08-06 王叔和生物医药(武汉)有限公司 硫氰酸钠在氧化间苯二酚合成制备噻克索酮中的应用及噻克索酮的制备方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CS103091A3 (en) * 1991-04-12 1992-10-14 Ustav Organicke Chemie A Bioch Protected substituted benzhydrylamines as shoulders for the synthesis ofpeptides on solid phase, process of their preparation and use
CA2193228A1 (fr) * 1994-06-23 1996-01-04 Christopher Holmes Compose photolabiles et procedes pour leur utilisation
US6528275B1 (en) * 1996-04-24 2003-03-04 Peptide Therapeutics Limited Substrates and inhibitors of proteolytic enzymes
GB9621985D0 (en) * 1996-10-22 1996-12-18 Peptide Therapeutics Ltd A solid-phase technology for the preparation of libraries of bi-directally functionalised drug-like molecules

Also Published As

Publication number Publication date
WO1999026902A1 (fr) 1999-06-03
EP1034154A1 (fr) 2000-09-13
JP2001524457A (ja) 2001-12-04
AU1342099A (en) 1999-06-15
AU734992B2 (en) 2001-06-28

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Legal Events

Date Code Title Description
FZDE Discontinued