新型醋酸优力司特衍生物的合成  

Synthesis of Novel Ulipristal Acetate Derivatives

作　　者：陈正帮 甘海峰[1] 冯卫杨 黄雨[1] 郭凯[1] 

机构地区：[1]南京工业大学生物与制药工程学院,江苏南京211816

出　　处：《合成化学》2014年第5期698-701,共4页Chinese Journal of Synthetic Chemistry

基　　金：中国国家高技术研究发展计划863项目(2012AA02A701)

摘　　要：以3,20-双(亚乙二氧基)-17α-羟基-5α,10α-环氧-19-去甲基孕甾-9(11)-烯为起始原料,与芳基溴经格氏加成反应得3,20-双(亚乙二氧基)-5α,17α-羟基-11β-芳基-19-去甲基孕甾-9-烯(3a^3f);3a^3f经羰基脱保护、水分子消除和乙酰化反应合成了6个新型的醋酸优力司特衍生物,其结构经1H NMR,IR,MS和HR-ESIMS表征。3,20-Bis-ethyl-enedioxy-5 α, 17 α-hydroxy-11β-aryl-19-norpregne-9-ene （ 3a - 3f） were prepared by Grignard reaction of 3,20-bis-ethylenedioxy-17a-hydroxy-5α, 10α-epoxy-19-norpregne-9 （ 11 ） -ene with aryl bromide. Six novel Ulipristal acetate derivatives were synthesized by deprotection of carbonyl group and removal of a molecule water to form an olefinic bond and then acetylation from 3a - 3f. The structures were characterized by 1H NMR, IR, MS and HR-ESI-MS.

关 键 词：醋酸优力司特 格式反应 合成 

分 类 号：O629.2[理学—有机化学] O621.3[理学—化学]