Process for preparing voriconazole

Details Process for preparing voriconazole Process for preparing voriconazole

C - Chemistry, Metallurgy

07

D

C07D 403/10 (2006.01) C07D 249/08 (2006.01)

Patent

CA 2590687

Voriconazole is prepared by a process comprising condensing 1-(2,4- difluorophenyl)-2-(1H-1,2,4-triazole-1-yl)ethanone with 4-chloro-6-ethyl-5- fluoropyrimidine, in a ketone, ether, aliphatic hydrocarbon, or aromatic hydrocarbon solvent, to give (2R, 3S/2S,3R)-3-(4-chloro-5-fluoropyrimidin-6- yl)-2-(2,4-diflurophenyl)-1-(1H-1,2,4-triazole-1-yl)butan-2-ol.

L'invention concerne du voriconazole preparé au moyen d'un procédé consistant à condenser 1-(2,4-difluorophényl)-2-(1H-1,2,4-triazole-1-yl)éthanone avec 4-chloro-6-éthyl-5-fluoropyrimidine, dans une cétone, de l'ether, un hydrocarbure aliphatique, ou un solvant d'hydrocarbure aromatique, afin d'obtenir (2R, 3S/2S,3R)-3-(4-chloro-5-fluoropyrimidin-6-yl)-2-(2,4-diflurophényl)-1-(1H-1,2,4-triazole-1-yl)butan-2-ol.

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