伏立康唑中间体工艺优化

Voriconazole Intermediate Process Improvement

伏立康唑是新型抗真菌药,为氟康唑衍生物,(2R,3S/2S,3R)-3-(4-氯-5-氟嘧啶-6-基)-2-(2,4-二氟苯基)-1-(1H-1,2,4-三唑-1-基)丁-2-盐酸盐是关键中间体,文章对合成该产品的路线进行优化,对不同的催化剂进行了比较,选择了成本比较低的氯化锌和三甲基氯硅烷混合催化剂,对温度、溶剂、原料配比等进行了优化,最终得到适合规模化生产的工艺。

Voriconazole is a novel antifungal drug.（2R, 3S/2S, 3R）-3-（4-chloro-5–fluoroprrimidin-6yl-）-2-（2,4-difluorophenyl）-1-（1H-1,2,4-triazol-1-yl）butan-2-ol hydrochloride is the key intermediate, the paper on the route research, choose zinc chloride and trimethylchlorosilane mixed catalyst, optimize the process, the temperature and the ratio of raw materials and processing, finally be suitable for large-scale production process.