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丙酸氟替卡松的合成工艺改进
引用本文:殷莉梅,韩静,张玥,杨静,潘岳峰. 丙酸氟替卡松的合成工艺改进[J]. 中国药物化学杂志, 2010, 19(1): 29-31,52
作者姓名:殷莉梅  韩静  张玥  杨静  潘岳峰
作者单位:沈阳药科大学 制药工程学院,辽宁 沈阳110016
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和核磁共振谱确证,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。

关 键 词:丙酸氟替卡松  醋酸地塞米松  氟米松  制备
收稿时间:2009-04-27
修稿时间:2009-07-20

Improved synthesis of fluticasone propionate
YIN Li-mei,HAN Jing,ZHANG Yue,YANG Jing,PAN Yue-feng. Improved synthesis of fluticasone propionate[J]. Chinese Journal of Medicinal Chemistry, 2010, 19(1): 29-31,52
Authors:YIN Li-mei  HAN Jing  ZHANG Yue  YANG Jing  PAN Yue-feng
Affiliation:YIN Li-mei,HAN Jing,ZHANG Yue,YANG Jing,PAN Yue-feng(School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,China)
Abstract:
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 1H-NMR,the content was greater than 98 % ditected by HPLC according to the European Pharmacopia.Conclusion Fluticasone propionate was prepared by dexam...
Keywords:fluticasone propionate  dexamethasone acetate  flumethasone  synthesis
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