【摘要】 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。更多还原

【Abstract】 5-(thiophen-2-yl)-2-p-tolyloxazole was synthesized via an oxidative cyclization reaction between 2-bromo-1-(thiophen-2-yl)-1-ethanone and p-tolylmethanamine in the presence of a catalyst amount of iodine and tert-butyl hydroperoxide(TBHP). The structure of the targeted product was confirmed by FTIR,NMR and MS,and biological activity of the product was tested. The results indicated that the optimum synthetic conditions were determined as follows:the amount of 2-bromo-1-(thiophen-2-yl)-1-ethanone,p-tolylmethanamine,iodine,TBHP(mass fraction 55%) and sodium bicarbonate was 1 mmol,1. 3 mmol,0. 2 mmol,1. 2 mmol and 1. 0 mmol,respectively,at room temperature for 12 h. The yield of the product reached 89. 7% under the above synthetic condition. The zone of inhibition showed that compound Ⅲ,the bacteriostatic diameters against Escherichia coli were21. 9 mm,exhibited a remarkable antibacterial activity.更多还原