发明名称 |
AN IMPROVED RILPIVIRINE PROCESS |
摘要 |
Disclosed is process for 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 |
EP2643294(B1) |
申请公布日期 |
2016.08.24 |
申请号 |
EP20120774414 |
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;C07C269/06;C07C271/28;C07D239/04;C07D239/48 |
主分类号 |
C07C255/34 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|