芳香杂环甲酰胺类化合物的合成研究

Synthesis of Aromatic Heterocyclic Formamide Compounds

研究重要中间体芳杂环甲酰胺类化合物合成的新方法。用溴代芳杂环类化合物与甲酰胺为原料,以便宜易得的氧化铜为催化剂,在缚酸剂的存在的情况下进行反应合成目标化合物。并探讨反应时间、反应温度、加入原料的物质的量比[n(溴代芳杂环类化合物)︰n(甲酰胺)]等因素对目标化合物产率的影响。最后以最优化条件得到芳杂环酰胺类化合物,最佳条件为:n(溴代芳杂环)︰n(甲酰胺)=1︰25,反应时间为8h,反应温度为120℃。并合成一系列有代表性的芳杂环酰胺类化合物,其结构经1 H NMR和13 C NMR确证。该路线工艺流程简单、快速,三废少且易处理,适合工业化生产。

A new method for the synthesis of important intermediate aryl heterocyclic formamide compounds was studied.The target compound was synthesized by bromination of aromatic heterocyclic compounds and formamide as the raw material and copper oxide as catalyst and the presence of acid binding agent.The effects of reaction time,reaction temperature and molar ratio of raw materials（bromo aromatic heterocyclic compounds,formamide）on the yield of target compounds were investigated.Finally,the optimum conditions were obtained for aromatic heterocyclic amide compounds.The optimum conditions were as follows：molar ratio of raw materials[n（bromo aromatic heterocycle）∶n（formamide）]=1∶25,reaction time was 8 h,reaction temperature was 120 ℃.A series of representative heterocyclic amide compounds were synthesized,and their structures were confirmed by ~1H NMR and ^（13）C NMR.The process is simple and fast,less waste and easy processing.