发明名称 |
PROCESS FOR PREPARATION OF RILPIVIRINE INTERMEDIATE |
摘要 |
<p>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-l-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%.</p> |
申请公布号 |
KR20130143046(A) |
申请公布日期 |
2013.12.30 |
申请号 |
KR20137011114 |
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 |
C07C253/30;C07C255/34;C07D239/04 |
主分类号 |
C07C253/30 |
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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