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AN IMPROVED PROCESS FOR THE PREPARATION OF BACLOFEN AND ITS INTERMEDIATE
专利权人:
发明人:
JAGTAP ASHUTOSH,GHARPURE MILIND,SHINDE NAVNATH,PATIL NAVNATH,RAUT CHANGDEV,KRISHNAMURTHY DHILEEPKUMAR
申请号:
IN2633/MUM/2015
公开号:
IN2015MU02633A
申请日:
2015.07.13
申请国别(地区):
IN
年份:
2017
代理人:
摘要:
The present invention provides an improved process for the preparation of 3-(4-chlorophenyl)-3- cyanopropanoic acid (compound (A)) and further its transformation to Baclofen (I). The process comprises reaction of compound (II) with Glyoxylic acid to obtain 3- (4-chlorophenyl)-3- cyanoacrylic acid (HI) followed by the in-situ reduction of (HI) in the presence of a reducing agent to provide the compound (A). Alternatively, the compound (A) is obtained by the process comprising reacting 2-(4- chlorophenyl)acetonitrile (II) with haloacetic acid (IV) in the presence of a base. The compound 3-(4-chlorophenyl)-3-cyanopropanoic acid (A) undergoes hydrogenation in the presence of a metal catalyst and ammonia solution to provide Baclofen (I).
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