Voriconazole → Voriconazole

Participants

Reaction Steps

More specifically, the invention relates to a process which comprises the dehalogenation of a haloderivative of Voriconazole via catalytic transfer hydrogenation of i.e (2R,3S/2S,3R)-3-(4-halo-5-fluoropyrimidin-6-yl)-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol to obtain racemic Voriconazole (i.e (2R,3S/2S,3R)-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol). Thereafter, racemic Voriconazole (compound V) is resolved using (1R)-(−)-10-camphorsulfonic acid ((−)-CSA) and isolating Voriconazole (compound I) from the diastereomeric salt Voriconazole (1R)-(−)-10-camphorsulfonate (compound VI).

Provenance & Evidence