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(1-苯乙基哌啶-4-基)苯胺(1)是合成阿片类镇痛药芬太尼(fentanyl)的重要中间体[1,2]。文献[3]以-苯乙胺和丙烯酸甲(乙)酯为原料,经Michael加成、Dieckmann缩合及酸性水解得N-苯乙基-4-哌啶酮(4),再与苯胺反应生成亚胺后由四氢锂铝还原得到1,总收率为30.5%～37.5%。4也可经三乙酰氧基硼氢化钠还原氨化[4]得到1。
(1-phenylethylpiperidin-4-yl) aniline (1) is an important intermediate for the synthesis of the opioid analgesic fentanyl [1,2]. Literature [3] - phenethylamine and methyl acrylate (meth) acrylate as raw materials, Michael addition, Dieckmann condensation and acid hydrolysis N-phenethyl-4-piperidone (4), and then react with aniline The imine is then reduced by lithium tetrahydroaluminate to give a total yield of 30.5% -37.5%. 4 can also be sodium triacetoxyborohydride reductive amination [4] 1.