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| 4-[（4-甲基哌嗪-1-基）甲基]苯甲酸二盐酸盐的合成研究 | |
| 引用本文： | 程锦涛,苏为科,徐斌. 4-[（4-甲基哌嗪-1-基）甲基]苯甲酸二盐酸盐的合成研究[J]. 广州化工, 2011, 39(9): 106-108 |
| 作者姓名： | 程锦涛 苏为科 徐斌 |
| 作者单位： | 1. 浙江工业大学,浙江,杭州,310000;台州知青化工有限公司,浙江,台州,318000 2. 浙江工业大学,浙江,杭州,310000 3. 台州知青化工有限公司,浙江,台州,318000 |
| 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%。 |
| 关 键 词： | 4-[（4-甲基哌嗪-1-基）甲基]苯甲酸二盐酸盐 甲磺酸依马替尼 合成 |
Synthesis of 4-[(4-Methyl-1-piperazinyl) methyl ] benzoic Acid Dihydrochloride HemihyDrate |
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| CHENG Jin-tao,SU Wei-ke,XU Bin. Synthesis of 4-[(4-Methyl-1-piperazinyl) methyl ] benzoic Acid Dihydrochloride HemihyDrate[J]. GuangZhou Chemical Industry and Technology, 2011, 39(9): 106-108 | |
| Authors: | CHENG Jin-tao SU Wei-ke XU Bin |
| Affiliation: | 1 Zhengjiang University of Technology,Zhengjiang Hangzhou 310000;2 Taizhou Zhiqing Chemical Co.,Ltd.,Zhengjiang Taizhou 318000,China) |
| Abstract: | 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%. |
| Keywords: | 1-(mercaptomethyl) cyclopropane acetic acid montelukast synthesis |
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