“一锅法”绿色合成N1-取代的3,4-二氢嘧啶酮衍生物

A green one-pot synthesis of N1-substituted 3,4-dihydropyrimidinones derivatives

在80℃、无溶剂条件下,以苯磺酸钐为催化剂,芳香醛、β-酮酯、N-取代的(硫)脲三组分“一锅法”缩合,较短的反应时间内合成了产率较高的N1-取代的3,4-二氢嘧啶酮衍生物。催化剂至少能重复使用三次。产品结构经IR,1H/13 C NMR,元素分析和X-射线单晶衍射进行了确证。与已报道的合成方法相比,该方法具有原料和催化剂用量少,产率高,方法绿色等优点。

The one-pot three-component condensation of aromatic aldehydes,β-ketoesters and N-substituted(thio)ureas in the presence of samarium benzenesulfonate had been accomplished under solvent-free conditions at 80℃.It afforded N1-substituted 3,4-dihydropyrimidinones derivatives with excellent yields in short reaction time.The catalyst could be reused at least three times.The structure of products was characterized by IR,1H/13 C NMR,elemental analysis and X-ray single crystal diffraction methods.Compared with the reported methods,this protocol had the advantages of small amount of raw materials and catalyst,high yield and green route,etc.