抗肿瘤药格列卫的合成工艺研究  

Synthesis of Antitummer Drug Gleevec

作　　者：刘昭文[1] 杨凯[1] 余磊[1] 吴龙火[1] 郭小华[1] 陈治希[1] 

机构地区：[1]赣南医学院药学院,江西赣州341000

出　　处：《化学试剂》2014年第6期574-576,共3页Chemical Reagents

摘　　要：采用2-溴-4-氨基甲苯为原料,与中间体4-(4-甲基哌嗪-1-甲基)苯甲酰氯发生酰胺化反应,继而与中间体4-(3-吡啶基)-2-氨基-嘧啶发生取代反应,最后与甲磺酸成盐共3步反应制得标题化合物。本路线操作简单、成本较低、条件温和、步骤少,适合工业化生产,总收率59.6%。Gleevec was synthesized from 3-Bromo-4-methylaniline and 4-（4-methyl-piperazin-l-ylmethyl）-benzoyl chloride and 4-Pyridin-3-yl-pyrimidin-2-ylamine via amidation and substitution reaction. This improved method can be used in industrial manufacturing with the advantage of simple purifying operation, lower cost and mild condition. The total yield was 59.6%.

关 键 词：格列卫 合成工艺 抗肿瘤药 

分 类 号：R979.1[医药卫生—药品]