17α－乙炔基－17β－羟基－18－甲基－△^（4，15）－雌甾二烯－3－酮（Gestodene）的合成研究  

Study on the Synthesis of 17α-ethynyl-17β-ol-18-methyl -△￣(4,15)-Estradiene-3-one (Gestodene)

作　　者：陈海林 陈建兴 陈良康 林锋 

机构地区：[1]上海计划生育科学研究所

出　　处：《生殖与避孕》1995年第3期197-201,共5页Reproduction and Contraception

摘　　要：以３－甲氧基－１７－羟基－１８－甲基雌甾－１，３，５（１０），８（９）－四烯（１１）为起始原料，经１１步反应制得Ｇｅｓｔｏｄｅｎｅ，总收率为３１％。运用澳化和脱溴化氢的化学方法引入关键的△１５双键结构，该方法所用试剂价廉易得，收率也较高，可作为Ｇｅｓｔｏｄｅｎｅ全合成的实用合成路线之一。Using, 3-methoxy-17-hydroxy-18-methyl-1,3,5(10), 8(9)-estratetraene (Ⅱ)as the starting material gestodene(Ⅰ)was obtained in a total yield of 31% through a series of 11 reactions. A key step was the introduction of a double bond in position 15 of the D-ring by bromination. and then dehydrobromination of compound 18-methoxy-17-cyclic (1, 2-ethanediyl acetal)-18-methyl-1, 3-5(10)-estratriene. This synthetic route is one of the practical methods for preparation of gestodene with available reagents and lower costs.

关 键 词：GESTODENE 上溴 脱溴 避孕药 合成 

分 类 号：R979.21[医药卫生—药品]