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Title:
PRODUCTION OF (2RS,3RS)-3-(2'-AMINOPHENYLTHIO)-2-HYDROXY-3-(4''-METHOXYPHENYL)-PROPIONIC ACID METHYL ESTER
Document Type and Number:
Japanese Patent JPH09132561
Kind Code:
A
Abstract:

To obtain the subject compound useful as a precursor for the production of diltiazem known as a pharmaceutically active substance in high stereoselectivity and yield.

The objective (2RS,3RS)-3-(2'-aminophenylthio)-2-hydroxy-3-(4''- methoxyphenyl)-propionic acid methyl ester can be produced by adding o- aminothiophenol of formula III to 3-(4'-methoxyphenyl)-grlycidic acid methyl ester of formula II in the presence of a weak acid alkali metal salt and a catalytic amount of an iron compound. The iron compound to be used in the reaction is e.g. an organic acid iron(III) sulfate and its amount of preferably 1-20ppm. The reaction temperature is preferably 90-120°C and the molar ratio of the compound of formula II to the compound of formula III is preferably 1:(0.9-1.1).


Inventors:
FUERUDEINANDO HAGEDORUN
HERUMUUTO FUIIGE
Application Number:
JP30865896A
Publication Date:
May 20, 1997
Filing Date:
November 06, 1996
Export Citation:
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Assignee:
BAYER AG
International Classes:
C07B53/00; C07C319/14; C07C319/18; C07C323/56; (IPC1-7): C07C323/56; C07B53/00; C07C319/14
Attorney, Agent or Firm:
Heiyoshi Odashima