| 摘要 |
Preparation of citalopram (I) comprises reacting a diphenylketone derivative (IV) with 3-(N,N-dimethylamino)propyl magnesium halide preferably 3-(N,N-dimethylamine)-propyl magnesium chloride and isolating (I) as the base or its salt. Preparation of citalopram of formula (I) comprises reacting a diphenylketone derivative of formula (IV) with 3-(N,N-dimethylamino)propyl magnesium halide preferably 3-(N,N-dimethylamine)-propyl magnesium chloride and isolating (I) as the base or its salt. [Image] R : 1-6C alkyl, 1-6C alkylsulfonyl or arylsulfonyl. Independent claims are included for the following: (1) preparation of a racemic compound of formula (III) which comprises deprotecting (IV) and reacting the obtained compound of formula (VIII) with 3-(N,N-dimethylamino)propyl magnesium halide, preferably 3-(N,N-dimethylamine)-propyl magnesium chloride and (2) new compounds (IV). [Image] - ACTIVITY : Antidepressant; nootropic. - MECHANISM OF ACTION : Serotonin (5-hydroxytryptamine; 5-HT) reuptake inhibitor.
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