- Synthetic method of voriconazole intermediate
-
The invention provides a synthetic method of a novel voriconazole intermediate condensation compound shown as a formula II or an acid addition salt thereof. The voriconazole intermediate is prepared by compounds shown as a formula III and a formula IV, the feeding way is adjusted, the reaction condition is moderate and controllable, the generation of an impurity A is reduced, the impurity A is controlled within 0.74 percent, the use of toxic metal lead is avoided, and the danger caused by the residue of toxic metal in a drug is eliminated; and the product purity is higher, and the industrial application value is high.
- -
-
Paragraph 0055; 0056
(2016/10/20)
-
- PROCESS FOR THE PREPARATION OF VORICONAZOLE AND INTERMEDIATES THEREOF
-
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.
- -
-
Paragraph 0038; 0039; 0040
(2014/12/09)
-
- PROCESS FOR PREPARING VORICONAZOLE BY USING NEW INTERMEDIATES
-
Provided is a process for preparing Voriconazole represented by Chemical Formula 1. More particularly, the process for preparing Voriconazole of Chemical Formula 1 includes: carrying out the Reformatsky-type coupling reaction between a ketone derivative of Chemical Formula 4 and a pyrimidine derivative of Chemical Formula 5 to obtain a compound of Chemical Formula 3; reacting the substituents halo and oxysulfonyl with a hydrogen donor to obtain racemicVoriconazole of Chemical Formula 2; and carrying out optical isolation of the racemicVoriconazole by adding an adequate optically active acid thereto to obtain Voriconazole having high optical purity with high cost-efficiency and high yield.
- -
-
Page/Page column 15-16
(2011/09/14)
-
