发明名称 |
IMPROVED PROCESS FOR PREPARING AN INTERMEDIATE FOR RILPIVIRINE SYNTHESIS |
摘要 |
The present invention relates to the preparation of a key Rilpivirine intermediate, namely (E)-4-(2-cyanoethenyl)-2,6-dimethylphenylamine hydrochloride (II) by a process comprising reaction of the tetrafluoroborate salt of the diazonium ion of 2,6-dimethyl-4-amino-1-carboxybenzyl phenylamine (VI) with acrylonitrile in presence of palladium acetate, followed by treatment with an acid and its subsequent conversion to the hydrochloride salt (II), wherein the undesired Z isomer is less than 0.5% and provides Rilpivirine hydrochloride having Z isomer less than 0.1%. |
申请公布号 |
EA024409(B1) |
申请公布日期 |
2016.09.30 |
申请号 |
EA20130001170 |
申请日期 |
2012.04.09 |
申请人 |
EMCURE PHARMACEUTICALS LIMITED |
发明人 |
GURJAR MUKUND, KESHAV;MAIKAP GOLAKCHANDRA, SUDARSHAN;JOSHI SHASHIKANT, GANGARAM;BADHE SACHIN, ARAVIND;MEHTA SAMIT, SATISH |
分类号 |
C07C255/34;C07C253/30;C07D239/04 |
主分类号 |
C07C255/34 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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