【摘要】 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(4%),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。更多还原

【Abstract】 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 chiral 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.更多还原