发明名称 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].
申请公布号 ZA200501254(B) 申请公布日期 2005.11.30
申请号 ZA20050001254 申请日期 2005.02.11
申请人 LES LABORATOIRES SERVIER 发明人 SOUVIE JEAN-CLAUDE;GONZALEZ BLANCO ISAAC
分类号 C07C;A61K;C07B61/00;C07C231/02;C07C233/18;C07C253/30;C07C253/34;C07C255/37;C07D 主分类号 C07C
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