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4-氯-3-(三氟甲基)苯异氰酸酯及其衍生物索拉菲尼的合成
Synthesis of 4-chloro-3-trifluoromethylaniline and sorafenib
【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)吡啶缩合成脲,制得抗肿瘤药物索拉菲尼,总收率为:84.0%,纯度:99.1%。
【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%.
【关键词】 4-氯-3-(三氟甲基)苯异氰酸酯;
索拉菲尼;
合成;
【Key words】 4-chloro-3-trifluoromethylaniline; sorafenib; synthesis;
【Key words】 4-chloro-3-trifluoromethylaniline; sorafenib; synthesis;
- 【文献出处】 化学工程师 ,Chemical Engineer , 编辑部邮箱 ,2011年01期
- 【分类号】TQ463.5
- 【被引频次】4
- 【下载频次】772