The reaction of α-tosyloxy ketones, sodium azide, and terminal alkynes in presence of copper(I) in aqueous polyethylene glycol afforded regioselectively 1,4-disubstituted 1,2,3-triazoles in good yield at ambient temperature. The one-pot exclusive formation of 1,4-disubstituted 1,2,3-triazoles involves in situ formation of α-azido ketones, followed by cycloaddition reaction with terminal alkyne. The
α-
甲苯磺酰氧基酮,
叠氮化
钠和末端炔在
铜(I)存在下在聚
乙二醇水溶液中反应在环境温度下以良好的产率提供区域选择性的1,4-二取代的
1,2,3-三唑。一锅独家形成1,4-二取代
1,2,3-三唑涉及原位形成α-
叠氮基酮,然后与末端
炔烃进行环加成反应。通过合成一系列不同的1,4-二取代的
1,2,3-三唑,证明了这种一锅法的普遍性。