(2β,3α,16β,17β)-3,17-双乙酰氧基-2,16-双哌啶基-5α-雄甾烷的合成
Synthesis of(2β,3α,16β,17β)-3,17-diacetoxy-2,16-dipiperidino-5α-androstane
作者:赖朋;马燕如;赵肖玉;徐正;
Author:
收稿日期: 年卷(期)页码:2006,(03):-258-260
期刊名称:华西药学杂志
Journal Name:WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字:雄甾烷类肌肉松弛药;泮库溴铵;维库溴铵;合成
Key words:
基金项目:
中文摘要
目的合成泮库溴铵和维库溴铵的中间体(2β,3α,16β,17β)-3,17-双乙酰氧基-2,16-双哌啶基-5α-雄甾烷。方法以表雄酮为原料,经磺酰化、消除、乙酰化、环氧化、取代、乙酰化反应合成目标化合物。结果所得产物及中间体经核磁共振谱确认。结论所设计合成路线可行,总收率30.4%,可用于工业生产。
参考文献
[1]WR Buckett,CL Hewett,DS Savage.Pancuronium bromide and othersteroidal neuromuscular blocking agents containing acetylcholine frag-ments[J].J Med Chem,1973,16:1116-1124.
[2]IC Carlyle,Sleigh Thomas,Savage David,et al.Acid addition salts of16-beta-monoquaternary ammonium derivatives of 2-beta,16-beta-bis-piperidino-androstanes and pharmaceutical preparationscontaining same[P].EP 8824.1980.
[3]李志达,郭文王景,何长云.抗肿瘤药环硫雄醇的合成[J].医药工业,1983,10:1-3.
[4]GC Wolf,RT Blickenstaff.Potential antiandrogenic antitumor steroidallactones[J].J Org Chem,1976,41(7):1254-1255.
[5]Z Tuba.Synthesis of 2β,16β-bis-(4’-dimethyl-1’-piperazino)-3α,17β-diacetoxy-5α-androstane Dibromide and Related Com-pounds[J].Arzneim-Forsch/Drug Res,1980,30(1):342-346.
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