| 4-氯-3-(三氟甲基)苯异氰酸酯及其衍生物索拉菲尼的合成 |
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| 引用本文： | 孙超,李彦辰,柳丽娜,徐赫,侯艳君.4-氯-3-(三氟甲基)苯异氰酸酯及其衍生物索拉菲尼的合成[J].化学工程师,2011(1):63-65. |
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| 作者姓名： | 孙超 李彦辰 柳丽娜 徐赫 侯艳君 |
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| 作者单位： | 《黑龙江大学化学化工与材料学院,黑龙江哈尔滨,150080 |
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| 摘 要： | 本文以邻氯三氟甲苯为起始原料,经混酸硝化,催化氢化,与BTC在1,2-二氯乙烷和1,4-二氧六环的混合溶剂中回流制得4-氯-3-(三氟甲基)苯异氰酸酯(三步总收率87.4%),再与4-(4-氨基苯氧基))-2-(甲基氨甲酰基)毗啶缩合成腺,制得抗肿瘤药物索拉菲尼.总收率为:84.0%.纯度:99.1%.
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| 关 键 词： | 4-氯-3-(三氟甲基)苯异氰酸酯 索拉菲尼 合成 |
Synthesis of 4-chloro-3-trifluoromethylaniline and sorafenib |
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| SUN Chao,LI Yan-chen,LIU Li-na,XU He,HOU Yan-jun.Synthesis of 4-chloro-3-trifluoromethylaniline and sorafenib[J].Chemical Engineer,2011(1):63-65. |
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| Authors: | SUN Chao LI Yan-chen LIU Li-na XU He HOU Yan-jun |
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| Affiliation: | (School of Chemical and Materials Science,Heilongjiang University,Harbin 150080,China) |
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| Abstract: | The target product was prepared from p-Chlorobenzotrifluoride（1）,which was transformed into the corresponding isocyanate（4） by mixed acid nitration,catalytic hydrogenation,and refluxed with BTC in the solution of 1,2-dichloroethane and 1,4-dioxare（the total yield of three steps was 87.4%）,then 4 reacted with 4-（4-aminophenoxy）-N-methyl-2-pyridinecarboxamide（5） to give the unsymmetrical diaryl urea sorafenib（6） as antitumor agent,the total yield was 84.0%,purity 99.1%. |
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| Keywords: | 4-chloro-3-trifluoromethylaniline sorafenib synthesis |
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