Process for the production of 2-[4-(3- and...

C - Chemistry – Metallurgy – 07 – C

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C07C 231/10 (2006.01) A61K 31/165 (2006.01) C07C 233/13 (2006.01)

Patent

CA 2653012

A process for obtaining therapeutically active 2-[4-(3- and 2- (fluorobenzyloxy)benzylamino]propanamides and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight. The process is carried out by submitting the Schiff bases intermediates 2- [4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to catalytic hydrogenation in the presence of a heterogeneous catalyst in a protic organic solvent.

La présente invention concerne un procédé pour obtenir des 2-[4-(3- et 2-(fluorobenzyloxy)benzylamino]propanamides thérapeutiquement actifs et leurs sels avec des acides pharmaceutiquement acceptables ayant un degré de grande pureté, en particulier, une teneur en impuretés de dérivés dibenzyle inférieure à 0,03 %, de préférence inférieure à 0,01 % en poids. Le procédé est effectué en soumettant les intermédiaires de bases de Schiff 2-[4-(3- et 2-fluorobenzyloxy)benzylidèneamino]propanamides à une hydrogénation catalytique en présence d'un catalyseur hétérogène dans un solvant organique protique.

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