罗库溴铵重要中间体17β-羟基-16β-四氢吡咯基雄甾-2(3)α-环氧化合物的合成工艺改进  

Improved synthesis of 2(3)α-epoxy-16β-(1-pyrrolidinyl)-androstan-17β-ol,main intermediate of Rocuronium bromide

作　　者：严昕[1] 许世卿[1] 陈瑛[1] 张倩[1] 夏鹏[1] 

机构地区：[1]复旦大学药学院药物化学教研室,上海200032

出　　处：《复旦学报（医学版）》2006年第6期851-853,共3页Fudan University Journal of Medical Sciences

摘　　要：目的改进罗库溴铵重要中间体17β-羟基-16β-四氢吡咯基雄甾-2(3)α-环氧化合物的合成工艺。方法对文献方法产生的副产物进行分离纯化和结构鉴定,根据所产生的副产物信息探索避免其形成的反应条件。结果优化了此步反应条件,避免专利条件下产生的副产物的生成,提高了反应收率。结论对17β-乙酰氧基雄甾-2(3)α,16(17)α-双环氧化物16位四氢吡咯开环反应专利方法下所得副产物进行了分离纯化和结构鉴定。根据此线索改进反应条件,使反应产物的纯化和收率得到显著提高。Purpose To improve the synthesis of 2（ 3 ）α-epoxy-16β-（1-pyrrolidinyl）-androstan-17β- ol, a main intermediate of Rocuronium bromide. Methods During examing patent method of this reaction, the undesired byproduct was isolated and its structure was identified by spectra. Based on this information, the reaction condition was improved by avoiding the form of the byproduct. Results The optimum reaction condition was obtained and the yield was raised. Conclusions The unreported byproduct from the patent reaction condition was isolated and confirmed. Improved reaction condition results in good yield.

关 键 词：药物化学 甾体 罗库溴铵 四氢吡咯 环氧开环 

分 类 号：TQ460.6[化学工程—制药化工]