5-三氟甲基-3-(4-甲基-1H-咪唑-1-基)苯胺的合成

Synthesis of 5-Trifluoromethyl-3-(4-methyl-1H-imidazol-1-yl)aniline

3,5-二硝基三氟甲苯(2)与氟化四甲铵进行氟代反应,所得单氟中间体再与4-甲基-1H-咪唑进行取代反应得到5-三氟甲基-3-(4-甲基-1H-咪唑-1-基)-硝基苯(3),然后在Pd/C催化下氢化还原制得抗肿瘤药尼罗替尼的中间体5-三氟甲基-3-(4-甲基-1H-咪唑-1-基)-苯胺(1),总收率约50%(以2计)。

5-Trifluoromethyl-3-（4-methyl-lH-imidazol-l-yl）aniline, the intermediate for antitumor agent nilotinib, was synthesized from 3,5-dinitro-l-trifluoromethylbenzene （2） by fluorination with tetramethyl ammonium fluoride to give 3-fluoro-5-trifluoromethyl-nitrobenzene, which was subjected to substitution with 4-methyl-lH-imidazole and reduction with an overall yield of about 50 %.