| 甲磺酸伊马替尼的合成 |
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| 引用本文： | 陈敖,黄荷香,宋帅娟,陈小琴.甲磺酸伊马替尼的合成[J].精细与专用化学品,2007,15(8):23-25. |
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| 作者姓名： | 陈敖 黄荷香 宋帅娟 陈小琴 |
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| 作者单位： | 丽珠集团常州康丽制药有限公司,江苏,常州,213105 |
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| 摘 要： | 以4-甲基-3-硝基苯胺为起始原料,经过缩合、还原、环合等反应制得抗肿瘤药物甲磺酸伊马替尼。并分别讨论了采用无水碳酸钾代替二异丙基乙胺、水合肼和普通催化剂代替铂炭催化剂以及采用异戊醇作为溶剂的优点。最终反应总收率超过50%,用高效液相色谱分析产品纯度在99.5%以上。
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| 关 键 词： | 4-甲基-3-硝基苯胺 甲磺酸伊马替尼 异戊醇 |
| 修稿时间： | 2007年1月5日 |
Synthesis of Imatinib Mesylate |
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| CHEN Ao,HUANG He-xiang,SONG Shuai-juan,CHEN Xiao-qin.Synthesis of Imatinib Mesylate[J].Fine and Specialty Chemicals,2007,15(8):23-25. |
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| Authors: | CHEN Ao HUANG He-xiang SONG Shuai-juan CHEN Xiao-qin |
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| Abstract: | The anticancer medicine imatinib mesylate was synthesized through steps composed of condensation, reduction and cyclization reaction using 4-methyl-3-nitroaniline as raw material. The advantages of using anhydrous potassium carbonate instead of diisopropylethylamine, replacing Pt/C catalyst with hydrazine hydrate and common catalyst, using isopentyl alcohol as solvent were discussed separately. Finally,the total yield was over 50% and purity of product was over 99.5% identified by HPLC. |
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| Keywords: | 4-methyl-3-nitroaniline imatinib mesylate isopentyl alcohol |
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