C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 405/12 (2006.01) A61K 31/445 (2006.01) A61K 31/4525 (2006.01) A61P 25/24 (2006.01) C07B 63/02 (2006.01) C07D 211/02 (2006.01) C07D 211/22 (2006.01)
Patent
CA 2457382
The present invention is directed to methods for preparing intermediates useful in the synthesis of paroxetine wherein the intermediates are substantially free of alkoxy impurities as well as to methods for preparing paroxetine and pharmaceutically acceptable salts thereof substantially free of alkoxy impurities. The alkoxy impurity is reacted with an ether cleaving agent to generate to corresponding phenol, which is separated, yielding the desired product substantially free of alkoxy impurities. Paroxetine intermediates such as PMA, paroxetine, and pharmaceutically acceptable salts thereof substantially free of alkoxy impurities also form part of the present invention.
L'invention concerne des procédés permettant la préparation de produits intermédiaires utiles pour la synthèse de la paroxétine, ces produits intermédiaires étant sensiblement exempts d'impuretés alcoxy, ainsi que des procédés permettant la préparation de paroxétine et de sels pharmaceutiquement acceptables de celle-ci, sensiblement exempts d'impuretés alcoxy. Ces procédés consistent à faire réagir l'impureté alcoxy avec un agent de clivage d'éther de manière à générer le phénol correspondant, et à séparer ce dernier de manière à obtenir le produit recherché sensiblement exempt d'impuretés alcoxy. L'invention concerne également les produits intermédiaires de la paroxétine tels que le PMA, la paroxétine et les sels pharmaceutiquement acceptables de celle-ci sensiblement exempts d'impuretés alcoxy.
Avrutov Ilya
Niddam-Hildesheim Valerie
Heenan Blaikie Llp
Teva Pharmaceutical Industries Ltd.
Teva Pharmaceuticals Usa Inc.
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