Process for the preparation of voriconazole and intermediates thereof
OwnerNitin Maheshwari, Roshan Ramesh Medhane +2inventors
InventorsNitin Maheshwari, Roshan Ramesh Medhane, Mohan Prasd, Sudershan Kumar Arora
Life of this patent
Estimating the term…
Abstract
The present invention relates to an improved stereoselective process for the preparation of (2R,3S/2S,3R)-3-(4-chloro-5-fluoropyrimidin-6-yl)-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol intermediate compound. This intermediate compound is further used to prepare voriconazole—a triazole antifungal agent.
Claims7
A stereoselective process for the preparation of (2R,3S/2S,3R)-3-(4-chloro-5-fluoropyrimidin-6-yl)-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol intermediate compound of Formula II or an acid addition salt thereof
- comprising the step of reacting 1-(2,4-difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone compound of Formula III
- with 6-(1-bromoethyl)-4-chloro-5-fluoropyrimidine compound of Formula IV
- in the presence of zinc, bromine and an aprotic organic solvent.
A process for the preparation of voriconazole comprising the step of reacting 1-(2,4-difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone compound of Formula III
- with 6-(1-bromoethyl)-4-chloro-5-fluoropyrimidine compound of Formula IV
- in the presence of zinc, bromine and an aprotic organic solvent to obtain a compound of Formula II or an acid addition salt thereof.
Dependencies are inferred from the claim text.