PROCESS FOR THE SYNTHESIS OF (7-METHOXY-3,4-DIHYDRO-1- NAPHTHALENYL) ACETONITRILE AND ITS APPLICATION IN THE SYNTHESIS OF AGOMELATINE

摘要

2-(7-Methoxy-3,4-dihydro-1-naphthyl)acetonitrile (I) is produced by reacting 7-methoxy-1-tetralone (IV) with cyanoacetic acid in the presence of an organoammonium carboxylate catalyst (VI) while removing water. 2-(7-Methoxy-3,4-dihydro-1-naphthyl)acetonitrile of formula (I) is produced by reacting 7-methoxy-1-tetralone (IV) with cyanoacetic acid in the presence of an organoammonium carboxylate catalyst of formula (VI) while removing water. R, R' : 3-10C alkyl, aryl or aryl(1-6C)alkyl, where aryl is phenyl, naphthyl or biphenylyl optionally substituted with 1-3 of 1-6C alkyl, OH and 1-6C alkoxy. An independent claim is also included for production of agomelatine, comprising producing (I) as above followed by aromatization, reduction and reaction with acetic anhydride. [Image].