Verfahren zur Herstellung von N-Methyl-3-(p-Trifluoromethyl-phenoxy)-3-phenyl-propylamin und ihre Salze

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), or a pharmaceutically acceptable acid addition salt thereof, characterized in that 2-benz...

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Bibliographische Detailangaben
Hauptverfasser: KAIRISALO, PEKKA JUHANI, SF-00950 HELSINKI, HUKKA, PETRI JUHANI, SF-02170 ESPOO, JAERVINEN, ANITTA HANNELE, SF-00960 HELSINKI
Format: Patent
Sprache:ger
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Zusammenfassung: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), or a pharmaceutically acceptable acid addition salt thereof, characterized in that 2-benzoyl-N-benzyl-N-methylethylamine base of formula (II), is hydrogenated catalytically, whereby 1-phenyl-3-(N-methylamino)propane-1-ol of formula (III) is formed, which is thereafter etherified selectively with 1-chloro-4-trifluoromethylbenzene of formula (IV), 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.