摘要
以N-甲基哌嗪及对氰基氯苄为起始原料,经缩合、水解两步反应合成甲磺酸依马替尼的关键中间体4-[(4-甲基哌嗪-1-基)甲基]苯甲酸二盐酸。重点对N-甲基哌嗪用量、水解反应时间和碱液浓度进行了考察,经优化后两步总收率达到76.2%。
4-[（4-methyl-1-piperazinyl）methyl]benzoic acid dihydrochloride hemihydrate,the key intermediate of imatinib mesylate,was prepared from 4-（Chloromethyl）benzonitrile and N-methyl piperazine by aldol reaction and hydrolytic reaction.Focus on the amount of N-methyl piperazine,the reaction time and alkali concentration were studied,and the optimized two-step total yield was 76.2%.
出处
《广州化工》
CAS
2011年第9期106-108,共3页
GuangZhou Chemical Industry
