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阿那曲唑的合成工艺改进
引用本文:隽海龙,王 静.阿那曲唑的合成工艺改进[J].药学与临床研究,2016,24(2):137-138.
作者姓名:隽海龙  王 静
作者单位:江苏正大清江制药有限公司,淮安,223005
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%。

关 键 词:阿那曲唑  相转移催化  合成
收稿时间:2015/7/29 0:00:00
修稿时间:2016/2/19 0:00:00

An Improved Synthesis Process for Anastrozole
JUAN Hai-long and WANG Jing.An Improved Synthesis Process for Anastrozole[J].Pharmacertical and Clinical Research,2016,24(2):137-138.
Authors:JUAN Hai-long and WANG Jing
Abstract: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%.
Keywords:Anastrozole  Phase transfer catalyst  Synthesis
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