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METHOD FOR PREPARING VORICONAZOLE L-CAMPHORSULPHONATE AND VORICONAZOLE

机译:制备伏立康唑L-樟脑硫酸和伏立康唑的方法

摘要

A method for preparing voriconazole L-camphorsulphonate and voriconazole. The method for preparing voriconazole L-camphorsulphonate comprises: method 1: dissolving (2R,3S)/(2S,3R) isomer mixture and L-camphor sulphonic acid in water and acetone, and performing crystallisation filtration to obtain voriconazole L-camphorsulphonate; method 2: (a) dissolving a mixture of isomer mixture and L-camphor sulphonic acid in a first solvent and then performing crystallisation filtration; or (a′) dissolving L-camphorsulphonate of the isomer mixture in a first solvent and then performing crystallisation filtration; (b) concentrating the filtrate obtained in step (a) or (a′) into a solid; and (c) dissolving the solid obtained in step (b) in a second solvent and performing crystallisation filtration to obtain voriconazole L-camphorsulphonate. Adjusting the resolution solvent effectively reduces production costs and facilitates recycling of the resolution solvent.
机译:一种制备伏立康唑L-樟脑硫酸和伏立康唑的方法。 制备voriconazole L-樟脑属的方法包括:方法1:溶解(2R,3S)/(2S,3R)异构体混合物和L-樟脑磺酸,并进行结晶过滤,得到伏立康唑L-樟脑硫酸盐; 方法2:(a)将异构体混合物和L-樟脑磺酸的混合物溶解在第一溶剂中,然后进行结晶过滤; 或(a')将异构体混合物的L-樟脑溶解在第一溶剂中,然后进行结晶过滤; (b)将步骤(a)或(a')中得到的滤液浓缩成固体; (c)将步骤(b)中获得的固体溶解在第二溶剂中并进行结晶过滤以获得voriconazole l-樟脑硫酸盐。 调节分辨率溶剂有效降低生产成本并促进分辨率溶剂的再循环。

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