摘要
目的:建立异甾体化合物I C_(13)位伯醇选择性氧化成α醛基的方法。方法:分别采用莫发特氧化(Moffatt Oxidation)、斯文氧化(Swern Oxidation)和氯铬酸吡啶盐(PCC)进行氧化反应。结果:三种氧化方法都能较好的将C_(13)位伯醇氧化成醛基,但在收率和醛基α、β构型比例上有所不同。结论:斯文氧化是一种高效、简便的氧化方法,能选择性的将C_(13)位伯醇氧化成目标α醛基产物,可作为异甾体化合物C_(13)伯醇氧化的可靠方法。
Objective : To establish an optimal method for selective oxidation of 13-hydroxymethyl of isosteroidal derivative 1 into or-aldehyde. Method: Oxidation procedure was respectively investigated by Moffatt Oxidation, Swern Oxidation and PCC reagent. Result: The conversion from 13-hydroxymethyl into aldehyde was achieved by all these three methods with different yields and isomeric ratios. Conclusion: Swern Oxidation is proved to be an efficient and convenient oxidation method, by which 13-hydroxymethyl can be selectively converted into ct-aldehyde. It can be used as a reliable method for primary alcohols.
出处
《中国药师》
CAS
2009年第8期1003-1005,共3页
China Pharmacist
基金
湖北省自然科学基金重点项目(2008CDA046)