丙酸氟替卡松的合成工艺改进  

Improved synthesis of fluticasone propionate

作　　者：殷莉梅[1] 韩静[1] 张玥[1] 杨静[1] 潘岳峰[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《中国药物化学杂志》2010年第1期29-31,52,共4页Chinese Journal of Medicinal Chemistry

摘　　要：目的制备丙酸氟替卡松。方法以醋酸地塞米松为原料,经乙酰化、氟化、水解3步反应制得中间体双氟米松,该中间体再通过氧化、巯基化、酯化、氟甲基化反应制得目标化合物。结果目标化合物的结构经质谱、核磁共振谱确证,总收率为52.85%,高效液相色谱检测含量大于98%。结论由醋酸地塞米松成功地制备丙酸氟替卡松,且有较好的收率和纯度,该工艺路线成本较低,操作简单。Aim To synthesize fluticasone propionate. Methods Fluoride betamethasone was prepared from dexamethasone acetate by acetylation, fluorination, hydrolysis. And the target compound was prepared by oxidation, sulfhydrylation, esterification, and fluoromethylation. Results The total yield is 52. 85%. The chemical structure of fluticasone propionate was confirmed by MS and ~H-NMR, the content was greater than 98 % ditected by HPLC according to the European Pharmacopia. Conclusion Fluticasone propionate was prepared by dexamethasone acetate successfully. This method is simple with lower cost, satisfied purity, and better and stable yield.

关 键 词：丙酸氟替卡松 醋酸地塞米松 氟米松 工艺改进 

分 类 号：R914[医药卫生—药物化学]