西替考马合成路线的优化  

The improvement for synthesis of centchroman

作　　者：季小慎[1,2] 金涛[1,2] 刘延苗 奕宋鹏 

机构地区：[1]空军总医院药理科药物化学室 [2]北京市医药药品公司

出　　处：《中国药学杂志》1998年第2期109-109,共1页Chinese Pharmaceutical Journal

摘　　要：目的：优化西替考马的合成路线、简化操作方法和提高反应产率。方法：通过改变反应起始物，重新设计反应路线。特别是利用２，２二甲基３苯基７甲氧基苯并吡喃（２）中的双键和苯酚进行ＦｒｉｅｄｅｌＣｒａｆｔｓ烷基化反应。结果：以五步反应获到最终产物。其中在ＦｒｉｅｄｅｌＣｒａｆｔｓ烷基化反应中高选择性的获得反式异构体，总收率达４０％。结论：避免了文献报道中的高压氢化和构型转化两个反应单元，简化了合成路线并提高了反应产率。OBJECTIVE: To improve the synthesis and promote the yield for centchroman. METHODS: The reported synthetic route was simplified and redesigned, especially using 2, 2dimethyl3phenyl7methoxychromene (2) to react with phenol. RESULTS: The transisomer was got in the step of highly stereoselective FriedelCrafts alkylation and final product centchroman was got just by five steps with over all yield of 40%. CONCLUSION: The synthesis for centchroman was simplified and yield was increased with out two steps of hydrogenation in high pressure and configuration transformation which appeared in the reported route.

关 键 词：西替考马 技术优化 合成路线 

分 类 号：TQ463.5[化学工程—制药化工]