Process for the preparation of...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 295/088 (2006.01) A61K 31/495 (2006.01)

Patent

CA 2454564

The present invention relates to a process for the manufacture of 2-{2-[4- (bis(4-fluorophenyl)methyl)-1-piperazinyl]ethoxy}acetic acids, amides or related derivatives, of the general formula (I) wherein: Y represents hydroxy or -NR1R2; R1 and R2 each independently represent hydrogen or C1-4#191 alkyl; m is 1 or 2, and n is 1 or 2, as well as the non-toxic, pharmaceutically acceptable salts and mixtures thereof. The present invention concerns also a polymorphic form of efletirizine.

La présente invention concerne un procédé de fabrication d'acides 2-(2-(4-(bis(4-fluorophényl)méthyl)-pipérazinyl)éthoxy)acétiques, d'amides ou de dérivés correspondants de la formule générale (1) dans laquelle Y est hydroxy ou -NR¿1?R¿2? ; R¿1? et R¿2? sont indépendamment hydrogène ou C?1-4¿alkyl ; m est 1 ou 2 ; et, n est 1 ou 2. L'invention concerne également les sels et mélanges non toxiques, pharmaceutiquement acceptables des composés selon l'invention. L'invention concerne par ailleurs une forme polymorphe d'éflétirizine.

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