度他雄胺的合成工艺  

Synthetic process of dutasteride

作　　者：边延林[1] 杨玉雷[1] 袁哲东[1] 

机构地区：[1]上海医药工业研究院创新药物与制药工艺国家重点实验室,上海200437

出　　处：《中国新药杂志》2011年第20期1972-1974,共3页Chinese Journal of New Drugs

基　　金：国家"重大新药创制"科技重大专项(2009ZX09301-007)

摘　　要：目的:确定并优化抗前列腺增生药物度他雄胺的合成工艺。方法:以羧酸黄体酮为原料,经氧化开环、环合、还原氢化、碘代、脱碘化氢、缩合6步反应得到度他雄胺。结果:本研究革除了原文献中毒性较大、价格较贵的试剂,并摸索后处理的方法,革除柱层析,通过六步反应合成目标化合物,降低了成本,简化了操作,合成总收率32.6%,纯度99.89%。结论:本方法成本低,操作简单,收率高,适合工业化生产。Objective： To optimize the synthetic process of dutasteride.Methods： Dutasteride was synthesized from 3-oxo-4-androstene-17β-carboxylic acid via six steps,including oxidative ring-opening,cyclization,reduction,iodination,dehydroiodination and finally acylation.Results： Our process abolished the toxic and expensive reagents reported in the primary literature.Meanwhile,we explored the method of purification to abolish column chromatography,which was of lower cost and easier operation.The overall yield was 32.6% with a purity of 99.89%.Conclusion： This synthetic process is of easy operation and low cost,which is suitable for industrialization.

关 键 词：度他雄胺 合成 5-Α还原酶抑制剂 

分 类 号：R914.5[医药卫生—药物化学]