PROCESS FOR RILPIVIRINE USING NOVEL INTERMEDIATE

摘要

The present invention provides a commercially viable process for preparing rilpivirine and its pharmaceutically acceptable acid addition salts thereof in high yields using novel intermediate.

主权项

1. A process for the preparation of rilpivirine of formula I: or a pharmaceutically acceptable salt thereof, which comprises:
a. reacting the 2,4-dichloropyrimidine of formula II: with (E)-3-(4-amino-3,5-dimethylphenyl)acrylonitrile hydrochloride of formula III: in the presence of tertiary amine and a suitable solvent to give (E)-3-(4-(2-chloropyrimidin-4-ylamino)-3,5-dimethylphenyl)acrylonitrile of formula IV; and b. reacting the (E)-3-(4-(2-chloropyrimidin-4-ylamino)-3,5-dimethylphenyl)acrylonitrile of formula IV with 4-aminobenzonitrile of formula V in an acid and a solvent to give rilpivirine of formula I and optionally converting rilpivirine formed into the pharmaceutically acceptable acid addition salt of rilpivirine.