抗真菌新药伏立康唑的合成工艺优化  

Synthesis of a novel antifungal drug voriconazole

作　　者：佟丽华[1] 王丽媛[1] 李红钊[1] 

机构地区：[1]佳木斯大学化学与药学院,黑龙江佳木斯154007

出　　处：《中南药学》2010年第4期280-282,共3页Central South Pharmacy

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。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.

关 键 词：伏立康唑 抗真菌药 合成工艺 

分 类 号：R914.4[医药卫生—药物化学]