| 尼洛替尼的合成研究 |
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| 引用本文： | 禹艳坤,王超,刘爱霞,冀亚飞.尼洛替尼的合成研究[J].化学试剂,2011,33(3):266-268. |
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| 作者姓名： | 禹艳坤 王超 刘爱霞 冀亚飞 |
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| 作者单位： | 华东理工大学,药学院,上海,200237 |
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| 摘 要： | 3-乙酰基吡啶与N,N-二甲基甲酰胺二甲缩醛反应制得(E)-3-二甲胺基-1-(3-吡啶基)-2-丙烯-1-酮,接下来与硝酸胍环合得4-(3-吡啶基)-2-胺基嘧啶,然后与3-溴-4-甲基苯甲酸乙酯缩合再经水解反应制得关键中间体4-甲基-3-4-(3-吡啶基)-2-嘧啶基]胺基]苯甲酸.此关键中间体直接与3-三氟甲...
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| 关 键 词： | 尼洛替尼 酪氨酸激酶抑制剂 抗白血病药 合成 |
Synthesis of Nilotinib |
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| YU Yan-kun,WANG Chao,LIU Ai-xia,JI Ya-fei.Synthesis of Nilotinib[J].Chemical Reagents,2011,33(3):266-268. |
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| Authors: | YU Yan-kun WANG Chao LIU Ai-xia JI Ya-fei |
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| Affiliation: | YU Yan-kun,WANG Chao,LIU Ai-xia,JI Ya-fei(School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China) |
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| Abstract: | 3-Acetylpyridine reacted with N,N-dimethylformamide dimethyl acetal to form(E)-3-dimethylamino-1-(pyridin-3-yl)prop-2-en-1-one,which was cyclized with guanidine nitrate to obtain 4-(pyridin-3-yl)-2-aminopyrimidine.4 was condensed with ethyl 3-bromo-4-methylbenzoate followed by hydrolysis to provide the key intermediate 4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)benzoic acid.Finally,6 was directly amidated with 3-trifluoromethyl-5-(4-methyl-1H-imidazol-1-yl)-benzenamine to achieve the highly selective i... |
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| Keywords: | nilotinib tyrosine kinase inhibitor antileukemia drug synthesis |
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