Imrpoved recrystallization processes for obtaining anhydrous...

Details Imrpoved recrystallization processes for obtaining anhydrous... Imrpoved recrystallization processes for obtaining anhydrous...

C - Chemistry, Metallurgy

07

D

C07D 401/12 (2006.01) A61K 31/4439 (2006.01) A61P 1/04 (2006.01)

Patent

CA 2409044

A process for producing crystals of (R)-2-[[[3-methyl-4-(2,2,2- trifluoroethoxy)-2-pyridyl]methyl]-sulfinyl]benzimidazole .n'H2O (wherein n' is about 0 to about 0.1) or of a salt thereof, characterized by subjecting a solution or dispersion in an organic solvent of (R)-2-[[[3-methyl-4-(2,2,2- trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]benz-imidazole .nH2O (wherein n is about 0.1 to about 1.0) to crystallization to crystallize out the target compound. This process is a simple process by which an optically active sulfoxide derivative can be efficiently and industrially mass-produced in high yield while attaining an extremely high enantiomer excess.

L'invention concerne un procédé pour produire un cristal de (R)-2-[[[3-méthyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl] méthyl]-sulfinyl] benzimidazole ?.¿ n'H¿2?O (où n' va d'environ 0 à environ 0,1) ou d'un sel de celui-ci. L'invention est caractérisée en ce qu'une solution ou une dispersion dans un solvant organique de (R)-2-[[[3-méthyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl] méthyl]-sulfinyl] benzimidazole ?.¿ n'H¿2?O (où n' va d'environ 0 à environ 0,1) est soumise à cristallisation pour cristalliser le composé cible. C'est un procédé simple, selon lequel un dérivé de sulfoxyde optiquement actif peut être produit à haut rendement, à l'échelle industrielle, en atteignant un excès substantiel d'énantiomère.

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