盐酸雷洛昔芬的合成改进  

Improved synthesis of raloxifene hydrochloride

作　　者：宋艳玲[1] 赵燕芳[2] 孟艳秋[1] 宫平[2] 

机构地区：[1]沈阳化工学院制药工程教研室,沈阳110142 [2]沈阳药科大学制药工程学院,沈阳110016

出　　处：《中国新药杂志》2005年第7期882-884,共3页Chinese Journal of New Drugs

摘　　要：目的:优化盐酸雷洛昔芬的合成路线。方法:以3-甲氧基苯硫酚和4-甲氧基-α-溴代苯乙酮为起始原料,经取代反应,环合反应得到6-甲氧基-2-(4-乙酰氧基苯基)苯并[b]噻吩,再与4-[2-(1-哌啶基)乙氧基]苯甲酰氯盐酸盐发生Friedel-Crafts反应,然后发生脱甲基反应,最后经成盐反应,共5步主要反应制得目标产物。结果:目标化合物结构经红外光谱、核磁共振氢谱及质谱确证。结论:本方法反应条件温和,操作简便,并且提高了产率。Objective：To optimize the synthetic route of raloxifene hydrochloride.Methods：The target compound was synthesized from 3- methoxybenzenethiol and 4- methoxy-α- bromo acetophenone via five steps, including substitution, cyclization, Friedel-Crafts reaction, demethyl reaction and salt formation. Results： The structure of the target compound was confirmed by IR, ^1 H-NMR and MS. Conclusion： This synthetic route had a mild reaction condition and improved yield,and was easily controlled.

关 键 词：盐酸雷洛昔芬 合成路线 骨质疏松 药物治疗 

分 类 号：R914.5[医药卫生—药物化学] R971.1[医药卫生—药学]