Improved method for preparing opipramol

C - Chemistry – Metallurgy – 07 – D

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C07D 403/06 (2006.01) C07D 223/22 (2006.01) C07D 223/26 (2006.01)

Patent

CA 2204261

An improved method for preparing opipramol is disclosed, wherein iminostilbene is reacted with 1-bromo-3-chloropropane in the presence of a weak base selected from a hydrogen phosphate salt and an acetate salt and in the presence of a phase transfer agent to produce N-(3-halopropyl)iminostilbene, which is mixture of N-(3- chloropropyl)iminostilbene and N-(3-bromopropyl)iminostilbene, and then N-(3-halopropyl)iminostilbene is reacted with N-(2-hydroxyethyl)piperazine to form opipramol.

L'invention présente un procédé amélioré de préparation d'opipramol, consistant à faire réagir de l'iminostilbène avec du 1-bromo-3-chloropropane, en présence d'une base faible sélectionnée à partir d'un sel d'hydrogéno-phosphate ainsi que d'un sel d'acétate, et en présence d'un agent de transfert de phase, afin de produire du N-(3-halopropyl)iminostilbène, lequel est un mélange de N-(3-chloropropyl)iminostilbène et de N-(3-bromopropyl)iminostilbène. On fait alors réagir le N-(3-halopropyl)iminostilbène avec de la N-(2-hydroxyethyl) piperazine pour obtenir de l'opipramol.

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