Process for preparing voriconazole, new polymorphic form of intermediate thereof, and uses thereof
AssigneeMedichem, S.A.
InventorsMonica Benito, Elies Molins, Juan Contreras
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Abstract
The present invention relates to an improved process for preparation of Voriconazole and Voriconazole (1R)-(−)-10-camphorsulfonate.
Claims16
A process for the preparation of Voriconazole, by treating Voriconazole (1R)-(−)-10-camphorsulfonate with a non-chlorinated organic solvent and an aqueous alkaline solution, wherein the Voriconazole (1R)-(−)-10-camphorsulfonate is obtained by a process which comprises:
- (a) dehalogenation of
- under catalytic transfer hydrogenation by using a catalyst in a solvent, wherein the obtained racemic Voriconazole is not isolated,
- (b) reacting the racemic Voriconazole with (1R)-(−)-10-camphorsulfonic acid in methanol,
- (c) optionally drying the obtained Voriconazole (1R)-(−)-10-camphorsulfonate.
A process for the preparation of Voriconazole with a small particle size distribution, which comprises treating Voriconazole (1R)-(−)-10-camphorsulfonate in an aqueous solution with a base.
A process for the preparation of Voriconazole (1R)-(−)-10-camphorsulfonate which comprises:
- (a) dehalogenation of
- under catalytic transfer hydrogenation by using a catalyst in a solvent, wherein the obtained racemic Voriconazole is not isolated,
- (b) reacting the racemic Voriconazole with (1R)-(−)-10-camphorsulfonic acid in methanol,
- (c) optionally drying the obtained Voriconazole (1R)-(−)-10-camphorsulfonate.
Voriconazole (1R)-(−)-10-camphorsulfonate compound of Form B.
Use of Voriconazole (1R)-(−)-10-camphorsulfonate compound of Form B for the preparation of Voriconazole.
Dependencies are inferred from the claim text.