EP 0434743 A4 19910925 - METHODS FOR PREPARING CAPTOPRIL AND ITS ANALOGUES
Title (en)
METHODS FOR PREPARING CAPTOPRIL AND ITS ANALOGUES
Publication
Application
Priority
US 24420388 A 19880913
Abstract (en)
[origin: WO9002732A1] This invention relates to novel methods for converting a diastereomeric mixture of S-protected derivatives of an orally active inhibitor of an angiotensin-converting enzyme (ACE) and its analogues into its separate optically resolved diastereomeric components. Specifically the invention relates to methods for the preparation of optically purified captopril and its analogs from racemic precursors. This resolution process is achieved through the fractional crystallization of S-protected derivatives of captopril and its precursors, which derivatives are useful for the reason that they are (1) easily prepared from novel precursors, (2) resolvable to their optically purified stereoisomeric species and (3) convertible to non-derivatized stereoisomeric species which correspond to the pharmacologically active inhibitor and its analogues. Novel methods for preparing the derivatives and their precursors are also noted herein. In addition, the novel derivatives and their precursors are also described herein.
IPC 1-7
IPC 8 full level
A61K 31/397 (2006.01); A61K 31/40 (2006.01); A61K 31/401 (2006.01); A61P 43/00 (2006.01); C07D 205/04 (2006.01); C07D 207/16 (2006.01); C07D 211/60 (2006.01)
CPC (source: EP)
A61P 43/00 (2017.12); C07D 205/04 (2013.01); C07D 207/16 (2013.01); C07D 211/60 (2013.01)
Citation (search report)
- US 4105776 A 19780808 - ONDETTI MIGUEL ANGEL, et al
- GB 2066243 A 19810708 - SQUIBB & SONS INC
- US 4297282 A 19811027 - OHASHI NAOHITO, et al
- GB 2066252 A 19810708 - EGYT GYOGYSZERVEGYESZETI GYAR
- EP 0035336 A2 19810909 - WYETH JOHN & BROTHER LTD [GB]
- Tetrahedron, Vol. 33, No. 38, 1977, pages 2725-2736; S.H. WILEN et al.: "Strategies in optical resolutions", whole article; especially chapter 4 (pages 2730-2732); figure 2.
- See references of WO 9002732A1
Designated contracting state (EPC)
AT BE CH DE FR GB IT LI LU NL SE
DOCDB simple family (publication)
WO 9002732 A1 19900322; AU 4304789 A 19900402; EP 0434743 A1 19910703; EP 0434743 A4 19910925; IL 91581 A0 19900429; IL 91581 A 19930708; JP H04500673 A 19920206
DOCDB simple family (application)
US 8903960 W 19890912; AU 4304789 A 19890912; EP 89910744 A 19890912; IL 9158189 A 19890908; JP 51013189 A 19890912