Preparation of citalopram as antidepressant drug and for treating dementia and cerebrovascular disorders comprises reaction of a new intermediate with 3-(N,N-dimethylamino)propyl magnesium halide

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. - DETAILED DESCRIPTION - 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. - 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). - ACTIVITY - Antidepressant; nootropic. - MECHANISM OF ACTION - Serotonin (5-hydroxytryptamine; 5-HT) reuptake inhibitor.