新型阿那曲唑衍生物的合成  

Synthesis of Novel Anastrozole Derivatives

作　　者：李钰[1] 梁鹏云[1] 王立升[1] 刘旭[1] 杨华[1] 周中杰[1] 

机构地区：[1]广西大学化学化工学院,广西南宁530004

出　　处：《合成化学》2013年第4期450-453,共4页Chinese Journal of Synthetic Chemistry

基　　金：教育部留学归国人员科研启动基金[教外司留(2007)1108号]

摘　　要：以3,5-二溴甲苯为原料,经钯催化剂催化插羰成酯、格氏反应、氯代、氰化、溴代、N-烷基化六步反应合成了阿那曲唑(总收率55.2%)。保留阿那曲唑苯环的对称部分,对其进行结构修饰,合成了13个新型的阿那曲唑衍生物,其结构经1H NMR,IR和MS表征。Anastrozole in total yield of 55.2% was synthesized from 3,5-dibromotoluene by a six-step reaction.Thirteen novel anastrozole derivatives were designed and synthesized based on Anastrozole.The structures were characterized by 1H NMR,IR and MS.

关 键 词：阿那曲唑 芳香酶抑制剂 结构修饰 合成 

分 类 号：O625.67[理学—有机化学] R914.5[理学—化学]