阿那曲唑的合成工艺改进  

An Improved Synthesis Process for Anastrozole

作　　者：隽海龙 王静[1] 

机构地区：[1]江苏正大清江制药有限公司,淮安223005

出　　处：《药学与临床研究》2016年第2期137-138,共2页Pharmaceutical and Clinical Research

摘　　要：通过相转移催化反应合成阿那曲唑采用a,a,a',a',5-五甲基-1,3-苯二乙腈为起始原料,在溴化剂N-溴代丁二酰亚胺作用下溴化生成中间体3,5-二[(2,2-二甲基)氰基甲基]-溴甲基苯,所得溴代中间体进而与1,2,4-三氮唑在水及有机溶剂中采用相转移催化缩合生产阿那曲唑。总收率达75%。This is a method for the synthesis of anastrozole using phase transfer catalyst: the bromination reaction of a,a,a',a',5-pentamethyl-1,3-benzenediacetonitrile as the starting material with N-bromosuccinimide as the bromide reagent give the intermediate 3,5-bis [(2,2-dimethyl)-cyanic methyl]-bromo methyl bengene; then the intermediate was reacted with 1,2,4- triazole in water and organic solvents by phase transfer catalytic condensation to obtain anastrozole. The total yield was up to 75%.

关 键 词：阿那曲唑 相转移催化 合成 

分 类 号：R914.5[医药卫生—药物化学]