N-(4-羟基苯基)-2-(1H-咪唑-1-基)乙酰胺的合成

Synthesis of N-(4-Hydroxyphenyl)-2-(1H-imidazol-1-yl) acetamide

对硝基苯酚经铁粉/氯化铵还原得到对氨基苯酚,后者经氯乙酰化和N-烷基化反应合成N-(4-羟基苯基)-2-(1H-咪唑-1-基)乙酰胺。并考察了酰化以及N-烷基化等关键步骤的反应条件,较佳的反应条件为酰化反应以乙酸钠作为缚酸剂,反应温度20℃;N-烷基化以碳酸钾作为缚酸剂,碘化钠为催化剂。总收率31.4%,产物经过1H NMR和MS表征。

4-Nitrophenol was reduced with iron filings and ammonium chloride to give 4-hydroxyaniline followed by chloroacetylation and N-alkylation for paffording N-（4-hydroxyphenyl）-2-（1H-imidazol-1-yl）acetamide.The reaction conditions for chloroacetylation and N-alkylation were optimized as follows：for acetylation,sodium acetate as acid binding agent at 20 ℃;for N-alkylation,potassium carbonate as acid binding agent and sodium iodide as catalyst.The overall yield is 31.4% and the target compound was characterized by ^1H NMR and MS.