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PROCESS FOR PREPARATION OF ASENAPINE MALEATE
专利权人:
发明人:
SINGH GIRIJ PAL,SRIVASTAVA DHANANJAL,BHADWAL PARAMVIR,BHOR MALHARI D,JANGAM SONARAJ BHOLENATH
申请号:
IN508/MUM/2013
公开号:
IN2013MU00508A
申请日:
2013.02.21
申请国别(地区):
IN
年份:
2014
代理人:
摘要:
The present invention relates to a process for the preparation of asenapine maleate. The process of the present invention involves cyclization of 3-(5-chloro-2-phenoxyphenyl)-l-methylpyrrolidine-2,4-dione (II) to give ll-chloro-2-methyl-2,3-dihydro-lH- dibenzo[2,3:6,7]oxepino[45-C] pyrrol-1-one (III), reduction of compound (III) to give mixture of cis-(3a, 12b)-ll-chloro-2-methyl- 2,3,3a,12b-tetrahydro-lH-dibenzo[2,3:6,7]oxepino[455-C]pyrrol-l-one (IV) and trans-(3a. 12b)-ll-chIoro-2-methyl-2,3,3a,12b- tetrahydro-lH-dibenzo[2,3:6,7]oxepino[4,5-C]pyrrol-l-one (V), enrichment of trans isomer (V) in the mixture by isomerization of the cis isomer (IV), separation of cis isomer (IV) and trans isomer (V), reduction of trans isomer (V) to asenapine free base (VI) and treatment of asenapine free base (VI) with maleic acid.
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