抗真菌新药伏立康唑的合成工艺优化

目的优化伏立康唑的合成工艺。方法以6-乙基-5-氟-4-羟基嘧啶为原料，通过氯代、溴代、缩合、氢化等反应及手性拆分方法制得了伏立康唑。结果伏立康唑的总收率为25．3％，远远高于文献报道的收率（4Z），制得的伏立康唑经过重结晶得到色谱纯度〉99％的成品。结论本方法合成路线短，反应过程温和，产物收率较高，产品纯度好，适于工业化生产。

Synthesis of a novel antifungal drug voriconazole

Objective To optimize the synthesis technology of voriconazole. Methods Using the 6 ethyl-5 fluorine -4- hydroxyl pyrimidine as starting materials, after chlorization, bromination, condensation reaction, hydrogenation reaction and then ehiral separation, the product was obtained. Results The total yield was 25.3%, far more than 4%, which was reported in the literature. After recrystallization, the purity of the finished product was higher than 99%. Conclusion This route is short, with high yield and the reaction condition is mild. It is suitable for industrial production.