3β-羟基-15β,16β亚甲基-17β-螺(环氧乙烷)-雄甾-5-烯的合成  

Synthesis of 15β,16β-Methylene-spiro-17β-oxiranyl-3β-hydroxy-androta-5-ene

作　　者：何明华[1] 廖清江[2] 

机构地区：[1]广东医学院药学院药物化学教研室,广东东莞523808 [2]中国药科大学药物化学教研室,江苏南京210009

出　　处：《化工时刊》2008年第3期27-28,共2页Chemical Industry Times

摘　　要：三甲锍硫酸甲酯是一种新型的硫叶立德试剂,将其应用于医药中间体3β-羟基-15β,16β亚甲基-17β-螺(环氧乙烷)-雄甾-5-烯的合成中,使用三甲锍硫酸甲酯,其催化剂为固体粉末KOH,而不像其它硫叶立德试剂要用昂贵的NaH作催化剂。成功的合成了目标化合物。产率75.6%,反应条件温和,利于工业化生产,产物经IR,1H-NMR、13C-NMR、MS确定。Trimethylsulfonium methylsulfate was a new kind of sulfur ylide reagent, which was applied in the synthesis of 15β, 16β- Methylene - spiro - 17β- oxiranyl - 3β- hydroxy - androta - 5 - en. as drug intermediates using trimethylsulfonium methylsulfate as epoxidation reagent. KOH was used as catalyst, not as other sulfur ylide which needed precious catalyst Nail. Target compound was synthesized, yield 75.6 %. This synthetic process was suitable for industrial preparation by its convenient operation and mild reaction conditions. The structures were confirmed by IR, ^I H- NMR, MS, ^13 C- NMR- spectra.

关 键 词：三甲锍硫酸二甲酯 环氧化作用 甾体 

分 类 号：TQ463[化学工程—制药化工]