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-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%. |
申请人 |
EMCURE PHARMACEUTICALS LIMITED;GURJAR, MUKUND KESHAV;MAIKAP, GOLAKCHANDRA, SUDARSHAN;JOSHI, SHASHIKANT, GANGARAM;BADHE, SACHIN, ARAVIND;MEHTA SAMIT, SATISH |
发明人 |
GURJAR, MUKUND KESHAV;MAIKAP, GOLAKCHANDRA, SUDARSHAN;JOSHI, SHASHIKANT, GANGARAM;BADHE, SACHIN, ARAVIND;MEHTA SAMIT, SATISH |