欧司哌米芬的两步法合成工艺研究  

Two-step synthesis technology of ospemifene

作　　者：张丹[1] 兰静[2] 李玲[3] 罗振福[3] 张春雪[1] 

机构地区：[1]天津理工大学化学化工学院,天津300384 [2]天津市药品审评中心,天津300191 [3]天津药物研究院化学制药部,天津300193

出　　处：《现代药物与临床》2012年第4期351-352,共2页Drugs & Clinic

摘　　要：目的研究欧司哌米芬的合成工艺。方法以4-羟基二苯甲酮为原料,与2-溴乙醇发生威廉姆斯发应,再与3-氯苯丙酮发生麦克莫里反应,得到终产物欧司哌米芬。结果本工艺路线所得产品产率为70%,质量分数>99.5%。结论所得欧司哌米芬的合成工艺稳定,操作简单,适合工业化大生产。Objective To study the synthetic process of ospemifene. Methods Ospemifene was synthesized by the Williamson reaction with 4-hydroxybenzophenone as material base, reacted with 2-bromoethanol, and then by the Mcmurry reaction with 3-chloropropiophenone. Results The yield of ospemifene was 70%, and purity was above 99.5%. Conclusion The synthesis process of ospemifene is stable, simple, and suitable for industrial production.

关 键 词：欧司哌米芬 4-羟基二苯甲酮 两步法合成 

分 类 号：R914.2[医药卫生—药物化学]