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%.
出处
《药学与临床研究》
2016年第2期137-138,共2页
Pharmaceutical and Clinical Research
关键词
阿那曲唑
相转移催化
合成
Anastrozole
Phase transfer catalyst
Synthesis