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PROCEDURE FOR PREPARATION OF N-METHYL-3-(P-TRIFLUOROMETHYLPHENOXY)-3-PHENYL-PROPYLAMINE HYDROCHLORIDE
PROCEDURE FOR PREPARATION OF N-METHYL-3-(P-TRIFLUOROMETHYLPHENOXY)-3-PHENYL-PROPYLAMINE HYDROCHLORIDE
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机译:N-甲基-3-(对-三氟甲苯氧基)-3-苯基丙胺盐酸盐的制备方法
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摘要
An improved process for the preparation of a valuable drug. The present invention relates to an improved process for the preparation of N-methyl-3-(p-trifluoromethylphenoxy)-3-phenyl-propylamine of formula (I), CHEM or a pharmaceutically acceptable acid addition salt thereof, characterized in that 2-benzoyl-N-benzyl-N-methylethylamine base of formula (II), CHEM is hydrogenated catalytically, whereby 1-phenyl-3-(N-methylamino)propane-1-ol of formula (III) is formed, CHEM which is thereafter etherified selectively with 1-chloro-4-trifluoromethylbenzene of formula (IV), CHEM in the presence of a base, whereby N-methyl-3-(p-trifluoromethylphenoxy)-3-phenyl-propylamine is formed, which is optionally converted in a known manner into the acid addition salt of Fluoxetine, e.g. Fluoxetine hydrochloride. The yield of Fluoxetine hydrochloride is 85-87% of the theoretical yield.
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