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以2-溴-1-(2-噻吩)-1-乙酮(Ⅰ)和对甲基苯甲胺(Ⅱ)为原料,在碘与叔丁基过氧化氢(TBHP)的复合催化作用下,通过氧化环合反应合成了5-(2-噻吩)-2-对甲苯基口恶唑(Ⅲ)。产物结构经FTIR、NMR和MS表征,并对产物的生物活性进行了测试。结果显示:合成反应的最佳条件为n(Ⅰ)=1 mmol、n(Ⅱ)=1.3 mmol、n(I2)=0.2 mmol、n〔TBHP(质量分数55%)〕=1.2mmol、n(Na HCO3)=1.0 mmol,室温下反应12 h,产物收率为89.7%。抑菌圈测定结果显示:化合物Ⅲ对大肠杆菌的抑菌圈直径为21.9 mm,具有强的抑菌能力。
Using 2-bromo-1- (2-thiophene) -1-ethanone (Ⅰ) and p-methylbenzylamine (Ⅱ) as starting materials, under the combined catalysis of iodine and t-butyl hydroperoxide The 5- (2-thiophene) -2-p-toluyl oxazole (Ⅲ) was synthesized by oxidative cyclization reaction. The product structure was characterized by FTIR, NMR and MS, and the biological activity of the product was tested. The results showed that the optimum conditions for the synthesis reaction were as follows: n (Ⅰ) = 1 mmol, n (Ⅱ) = 1.3 mmol, n (I2) = 0.2 mmol, n [TBHP Na HCO3) = 1.0 mmol, reacted for 12 h at room temperature, the yield of the product was 89.7%. The results of inhibition zone showed that the inhibition zone diameter of compound Ⅲ to Escherichia coli was 21.9 mm and had strong antibacterial activity.