N-(4-氯-3-三氟甲基苯基)-N′-(4-溴苯基)脲的合成

Synthesis of N-(4-Chloro-3-trifluoromethylphenyl)-N′-(4-bromophenyl) urea

4-氯-3-三氟甲基苯胺和三光气在乙酸乙酯中反应制得4-氯-3-三氟甲基苯异氰酸酯,不经分离纯化,直接与对溴苯胺反应制得抗肿瘤药索拉非尼的中间体N-(4-氯-3-三氟甲基苯基)-N-(4-溴苯基)脲,总收率约75%,纯度99.8%。

N- （4-Chloro-3-trifluoromethylphenyl） -N＇- （4-bromophenyl） urea, a key intermediate of antitumor agent sorafenib was synthesized from 4-chloro-3-trifluoromethylaniline and triphosgene to give 4-chloro-3- trifluoromethyl phenyl isocyanate, which without seperation reacted with 4-bromoaniline in about 75 % overall yield and 99.8 % purity.