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WO2000053579A3 - Solid phase synthesis of 4-aminoproline derivatives and/or combinatorial libraries thereof - Google Patents

Solid phase synthesis of 4-aminoproline derivatives and/or combinatorial libraries thereof Download PDF

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Publication number
WO2000053579A3
WO2000053579A3 PCT/US2000/006021 US0006021W WO0053579A3 WO 2000053579 A3 WO2000053579 A3 WO 2000053579A3 US 0006021 W US0006021 W US 0006021W WO 0053579 A3 WO0053579 A3 WO 0053579A3
Authority
WO
WIPO (PCT)
Prior art keywords
formula
solid phase
phase synthesis
optionally substituted
aminoproline
Prior art date
Application number
PCT/US2000/006021
Other languages
French (fr)
Other versions
WO2000053579A2 (en
Inventor
Michael Douglas Hocker
Matthew Plunkett
Original Assignee
Axys Pharm Inc
Michael Douglas Hocker
Matthew Plunkett
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
Application filed by Axys Pharm Inc, Michael Douglas Hocker, Matthew Plunkett filed Critical Axys Pharm Inc
Priority to AU35174/00A priority Critical patent/AU3517400A/en
Publication of WO2000053579A2 publication Critical patent/WO2000053579A2/en
Publication of WO2000053579A3 publication Critical patent/WO2000053579A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

The present invention relates to solid phase synthesis of proline based compounds of Formula (1): R4R5NC(O)-Q-N(R1)-Y-R2 wherein R1 is an optionally substituted alkyl; R2 is alkyl, or optionally substituted aryl; R?4 and R5¿ are independently selected from cycloalkyl, or optionally substituted alkyl; R?4 and R5¿ taken together represent a five to seven membered saturated or unsaturated heterocyclic ring; Q represents (a) or (b), Y represents -S(O)¿n?-, -C(O)-, or -C(O)-NH-. Compounds of Formula (1) are prepared by a process which enables individual, parallel, and simultaneous synthesis of a plurality of compounds represented by Formula (1), starting from a compound of Formula (A): LG-C(O)-Z wherein LG represents a leaving group, Z represents (c), PG represents a protecting group.
PCT/US2000/006021 1999-03-10 2000-03-08 Solid phase synthesis of 4-aminoproline derivatives and/or combinatorial libraries thereof WO2000053579A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU35174/00A AU3517400A (en) 1999-03-10 2000-03-08 Proline derivatives and synthesis thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US12363199P 1999-03-10 1999-03-10
US60/123,631 1999-03-10

Publications (2)

Publication Number Publication Date
WO2000053579A2 WO2000053579A2 (en) 2000-09-14
WO2000053579A3 true WO2000053579A3 (en) 2000-12-21

Family

ID=22409844

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/006021 WO2000053579A2 (en) 1999-03-10 2000-03-08 Solid phase synthesis of 4-aminoproline derivatives and/or combinatorial libraries thereof

Country Status (2)

Country Link
AU (1) AU3517400A (en)
WO (1) WO2000053579A2 (en)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994024314A1 (en) * 1993-04-19 1994-10-27 Kauffman Stuart A Random chemistry for the generation of new compounds
WO1998020350A1 (en) * 1996-11-05 1998-05-14 Pharmacopeia, Inc. Combinatorial hydroxy-amino acid amide libraries

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994024314A1 (en) * 1993-04-19 1994-10-27 Kauffman Stuart A Random chemistry for the generation of new compounds
WO1998020350A1 (en) * 1996-11-05 1998-05-14 Pharmacopeia, Inc. Combinatorial hydroxy-amino acid amide libraries

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
BALKENHOHL F. ET AL.: "Combinatorial synthesis of small organic molecules", ANGEWANDTE CHEMIE. INTERNATIONAL EDITION, DE, VERLAG CHEMIE. WEINHEIM, vol. 35, no. 20, 1996, pages 2288 - 2337, XP002065423, ISSN: 0570-0833 *
BRAY A.M. ET AL.: "Rapid optimization of organic reactions on solid phase using the multipin approach: Synthesis of 4-aminoproline analogues by reductive amination", TETRAHEDRON LETTERS, NL, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, vol. 36, no. 28, 10 July 1995 (1995-07-10), pages 5081 - 5084, XP004027743, ISSN: 0040-4039 *
NEFZI A. ET AL.: "The current status of heterocyclic combinatorial libraries", CHEMICAL REVIEWS, US, AMERICAN CHEMICAL SOCIETY. EASTON, vol. 97, no. 2, 1 April 1997 (1997-04-01), pages 449 - 472, XP002144163 *
TERRETT N K ET AL: "Combinatorial synthesis - The design of compound libraries and their application to drug discovery", TETRAHEDRON, NL, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, vol. 51, no. 30, 24 July 1995 (1995-07-24), pages 8135 - 8173, XP000644580, ISSN: 0040-4020 *

Also Published As

Publication number Publication date
WO2000053579A2 (en) 2000-09-14
AU3517400A (en) 2000-09-28

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