Preparation procedure for rilpivirine using a new intermediate

摘要

Method of preparing rilpivirine of formula I: ** (See formula) ** or its pharmaceutically acceptable salts, comprising: a. react the 2,4-dichloropyrimidine of formula II: ** (See formula) ** with (E) -3- (4-amino-3,5-dimethylphenyl) acrylonitrile hydrochloride of formula III: ** (See formula) ** in the presence of a tertiary amine and a suitable solvent to obtain (E) -3- (4- (2-chloropyrimidin-4-ylamino) -3,5- 40 dimethylphenyl) acrylonitrile of formula IV; and ** (See formula) ** b. Reacting (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 obtain rilpivirine of formula I and optionally convert the obtained rilpivirine into a pharmaceutically acceptable acid addition salt of rilpivirine ** (See formula) **