FIELD: medicine. SUBSTANCE: described is method of preparing fluoxetin, more particularly N-methyl-{3-phenyl-3-[4-(trifluoromethyl)phenoxy] propyl amine of formula I: SSS and pharmaceutically acceptable acid addition salts by reaction of N,N-dimethyl-{3-phenyl-3-[4- (trifluoromethyl)phenoxy]propyl amine of formula III: SSS and ethylchloroformate, hydrolysis and decarboxylation of N-methyl-N- ethoxycarbonyl-{3-[4-trifluoromethyl)phenoxy]propyl} amine of formula II: SSS and optionally preparing salt. Method comprises reacting compound of formula III with ethylchloroformate in toluene or xylene or mixture thereof at temperature of lower than 90 C; removing mixture of impurities and by-products from reaction mixture by treating with dilute acid; separating organic phase containing urethane derivative of formula II with alkali metal hydroxide at boiling temperature of reaction mixture in the presence of water and optionally n-butanol; removing inorganic compounds and optionally converting the resulting base of formula I into pharmaceutically acceptable acid addition salt thereof. Compounds of formula I are known as useful antidepressants. EFFECT: simplified process. 8 cl
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Authors
Dates
2001-09-20—Published
1997-09-10—Filed