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度他雄胺的合成工艺
引用本文:张奎平,雷小平. 度他雄胺的合成工艺[J]. 中国药学, 2007, 16(3): 233-235
作者姓名:张奎平  雷小平
作者单位:北京大学药学院药物化学系 北京100083
摘    要:目的制备度他雄胺。方法孕烯酮醇经过酯化、氧化(沃氏反应)、水解得孕烯酮酸,再经过氧化开环、环合、还原、氧化、酰基化共八步制得目标产物。结果最终产物由核磁共振谱和元素分析进行结构鉴定。总收率为31.5%。结论探索了不同条件对各个合成中间体的产率的影响,找出合适的反应条件,使之更适于工业生产。

关 键 词:甾体激素  度他雄胺  孕烯酮醇  5-α还原酶抑制剂
文章编号:1003-1057(2007)3-233-03
修稿时间:2007-02-19

Synthesis of dutasteride
Kui-Ping Zhang,Xiao-Ping Lei. Synthesis of dutasteride[J]. Journal of Chinese Pharmaceutical Sciences, 2007, 16(3): 233-235
Authors:Kui-Ping Zhang  Xiao-Ping Lei
Affiliation:Peking University School of Pharmaceutical sciences, Beijing 100083, China;
Abstract:Aim To synthesize dutasteride. Methods The target compound was synthesized from pregnenolol via eight steps, in- cluding esterification, oxidation, hydrolysis, then oxidative ring-opening, cyclization, reduction, oxidization and finally acylation. Results The structure of the target molecule was identified by 1H NMR, 13C NMR and element analysis. The overall yield was 31.5%. Conclusion The effects of different reaction conditions on the yield of product in each step have been investigated and the optimal reaction conditions have been established.
Keywords:Steroid hormones  Dutasteride  Pregnenolol
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