孕甾-5-烯-3β,20-二取代硫酸酯钠盐的合成  

Synthesis of Disodium 3β,20-dihydroxypregn-5-ene Disulfate

作　　者：李莹[1] 王辉[1] 崔建国[1] 

机构地区：[1]广西师范学院化学与生命科学学院,广西南宁530001

出　　处：《广西师范学院学报（自然科学版）》2009年第2期52-54,共3页Journal of Guangxi Teachers Education University(Natural Science Edition)

基　　金：国家自然科学基金(批准号:20562001);广西科学基金(批准号:桂科基057554)资助

摘　　要：甾醇硫酸酯钠化合物由于其独特的结构特征和特殊的生理活性正引起人们越来越多的关注.从孕邕醇酮出发,在Ce3+离子存在下经过硼氢化钠还原得到孕甾-5-烯-3β,20-二醇(2),2利用三乙胺-三氧化硫复合物进行硫酸酯化,得到产物(3).然后3通过阳离子(钠型)交换树脂进行Na+交换得到目标产物孕甾-5-烯-3,β20-二取代硫酸酯钠(4).In recent years,the sodium polyhydroxysterols sulfated greatly attract the attention of organic chemists and biomedical scientists due to their novel structures and biological activities against cancer and micropathogens.Using pregnenolone（1） as starting material,disodium 3β,20-dihydroxypregn-5-ene disulfate（4） was synthesized in 3 steps with a high overall yield.First,pregnenolone（1） was transformed into pregn-5-en-3β,20-diol（2） with NaBH4 in the presence of CeCl3.The reaction of 2 with triethylamine-sulfur trioxide complex offered 3 and the treatment of 3 by Cation exchange resin 732 （sodium form） gave the target steroid 4. The compound 4 was assayed for antitumor activity in vitro against rome cancer cell plants and the result showed that there was no significant cytotoxicity.

关 键 词：甾醇 甾醇硫酸酯钠 孕甾-5-烯-3 β20-二取代硫酸酯钠 合成 

分 类 号：O629.29[理学—有机化学]