WO2003072042A3 - Malonate-claisen rearrangement for preparation of integrin receptor antagonist intermediates - Google Patents

Malonate-claisen rearrangement for preparation of integrin receptor antagonist intermediates Download PDF

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Publication number
WO2003072042A3
WO2003072042A3 PCT/US2003/005476 US0305476W WO03072042A3 WO 2003072042 A3 WO2003072042 A3 WO 2003072042A3 US 0305476 W US0305476 W US 0305476W WO 03072042 A3 WO03072042 A3 WO 03072042A3
Authority
WO
WIPO (PCT)
Prior art keywords
preparation
malonate
integrin receptor
claisen rearrangement
receptor antagonist
Prior art date
Application number
PCT/US2003/005476
Other languages
French (fr)
Other versions
WO2003072042A2 (en
Inventor
Guy R Humphrey
Roger N Farr
Jaemoon Lee
Original Assignee
Merck & Co Inc
Guy R Humphrey
Roger N Farr
Jaemoon Lee
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 Merck & Co Inc, Guy R Humphrey, Roger N Farr, Jaemoon Lee filed Critical Merck & Co Inc
Priority to AU2003216374A priority Critical patent/AU2003216374A1/en
Publication of WO2003072042A2 publication Critical patent/WO2003072042A2/en
Publication of WO2003072042A3 publication Critical patent/WO2003072042A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Abstract

A novel process is provided for the preparation of chiral unsaturated ester intermediates useful in the asymmetric syntheses of α νβ 3 integrin receptor antagonists. The instant process involves an efficient Claisen rearrangement of a malonate ester of a chiral allylic alcohol precursor followed by hydrolysis and decarboxylation. The unsaturated ester intermediates can be converted in a 2-step sequence into the desired substituted nonanoic acid derivatives.
PCT/US2003/005476 2002-02-27 2003-02-21 Malonate-claisen rearrangement for preparation of integrin receptor antagonist intermediates WO2003072042A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003216374A AU2003216374A1 (en) 2002-02-27 2003-02-21 Malonate-claisen rearrangement for preparation of integrin receptor antagonist intermediates

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US36027302P 2002-02-27 2002-02-27
US60/360,273 2002-02-27

Publications (2)

Publication Number Publication Date
WO2003072042A2 WO2003072042A2 (en) 2003-09-04
WO2003072042A3 true WO2003072042A3 (en) 2004-03-04

Family

ID=27766213

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/005476 WO2003072042A2 (en) 2002-02-27 2003-02-21 Malonate-claisen rearrangement for preparation of integrin receptor antagonist intermediates

Country Status (2)

Country Link
AU (1) AU2003216374A1 (en)
WO (1) WO2003072042A2 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI3929196T3 (en) 2013-09-24 2023-10-02 Fujifilm Corp Pharmaceutical composition of a nitrogen-containing compound or salt thereof, or metal complex thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6048861A (en) * 1997-12-17 2000-04-11 Merck & Co., Inc. Integrin receptor antagonists
US6444680B1 (en) * 2000-11-30 2002-09-03 Merck & Co., Inc. Amine salts of an integrin receptor antagonist

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6048861A (en) * 1997-12-17 2000-04-11 Merck & Co., Inc. Integrin receptor antagonists
US6444680B1 (en) * 2000-11-30 2002-09-03 Merck & Co., Inc. Amine salts of an integrin receptor antagonist

Also Published As

Publication number Publication date
AU2003216374A1 (en) 2003-09-09
WO2003072042A2 (en) 2003-09-04
AU2003216374A8 (en) 2003-09-09

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