A process for preparing duloxetine and intermediates for use...

Details A process for preparing duloxetine and intermediates for use... A process for preparing duloxetine and intermediates for use...

C - Chemistry, Metallurgy

07

D

C07D 333/20 (2006.01) A61K 31/381 (2006.01) A61P 25/24 (2006.01)

Patent

CA 2510750

A process for preparing (+)duloxetine, or an acid addition salt thereof, which process comprises resolving racemic (.plusmn.)duloxetine with a chiral acid so as to obtain a salt of the chiral acid and (+)duloxetine, substantially free of (-)duloxetine; and (ii) if desired, converting the salt prepared in step (i) to the free base or another acid addition salt as appropriate. The process for preparing (+)duloxetine, or an acid addition salt thereof, can further comprise an O-alkylation intermediate process step which is carried out in the presence of a base and a phase transfer catalyst.

L'invention concerne un procédé pour préparer la (+)duloxétine, ou un de ses sels d'addition d'acide, ledit procédé comprenant les étapes suivantes : décomposer la (.plusmn.)duloxétine racémique au moyen d'un acide chiral, de façon à obtenir un sel d'acide chiral et de la (+)duloxétine, sensiblement exempt de (-)duloxétine ; et (ii) si nécessaire, convertir le sel préparé dans l'étape (i) en une base libre ou tout autre sel d'addition d'acide approprié. Ledit procédé de préparation de la (+)duloxétine, ou un de ses sels d'addition d'acide, peut également comprendre une étape de procédé intermédiaire d'O-alkylation qui est effectuée en présence d'une base et d'un catalyseur de transfert de phase.

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