Preparation of n-methylparoxetine and related intermediate...

C - Chemistry – Metallurgy – 07 – D

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C07D 405/12 (2006.01) C07D 211/22 (2006.01) C07D 317/64 (2006.01)

Patent

CA 2437392

The present invention provides a process for preparing N-methylparoxetine, an intermediate in the synthesis of paroxetine, by reacting sesamol- tetrabutylammonium salt with CIPMA. The synthesis of the intermediate in the prior are resulted in a particularly low yield. The use of the sesamol- tetrabutylammonium salt increases the yield by more than three folds over the prior art. The present invention is not limited to the synthesis of N- methylparoxetine, but also includes other similar compounds.

La présente invention concerne un procédé de préparation de N-méthylparoxétine, un intermédiaire dans la synthèse de paroxétine, par la mise en réaction de sel de sésamol-tétrabutylammonium avec CIPMA. Dans la technique antérieure, le rendement de la synthèse de cet intermédiaire est particulièrement faible. L'utilisation de sel de sésamol-tétrabutylammonium augmente ce rendement de plus de trois fois par rapport à la technique antérieure. Ladite invention ne se limite pas à la synthèse de N-méthylparoxétine, mais concerne également d'autres composés similaires.

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