A process of preparing imatinib and imatinib prepared thereby

Details A process of preparing imatinib and imatinib prepared thereby A process of preparing imatinib and imatinib prepared thereby

C - Chemistry, Metallurgy

07

D

C07D 401/04 (2006.01) A61K 31/506 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2516370

A process of preparing imatinib, either as the free base or as an acid addition salt, which process comprises reacting N-(2-methyl-5-aminophenyl-4-(3- pyridyl)-2-pyrimidine amine of formula (II) with a 4-(4-methyl-piperazino methyl)benzoyl halide of formula (III) in the presence of an inert organic solvent, so as to yield a hydrohalide salt of imatini formula (I) where n represents 1, 2 or 3 and Hal represents bromo, chloro fluoro or iodo, either in anhydrous or hydrated form, which can as desired optionally be further conve either to the free base or a further acid addition salt. The present invention is also concerned with imatinib prepared according to the above process.

Procédé de préparation d~imatinibe, soit sous forme de base libre ou d~un sel d~addition d~acide, consistant à faire réagir une N-(2-méthyl-5-aminophényl-4-(3-pyridyl)-2-pyrimidine amine de formule (II) avec un halogènure 4-(4-méthyl-pipérazino méthyl) benzoyl de formule (III), en présence d~un solvant organique inerte, de manière à donner un sel halohydrate d~imatinibe de formule (I) où n représente 1, 2 ou 3 et Hal représente bromo, chloro fluoro ou iodo, sous forme anhydre ou hydratée, lequel sel peut si on le désire subir une nouvelle conversion pour donner la base libre ou un autre sel d~addition d~acide. La présente invention concerne également une imatinibe préparée selon ledit procédé.

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