Copper-Catalyzed Sulfonyl Azide–Alkyne Cycloaddition Reactions: Simultaneous Generation and Trapping of Copper–Triazoles and −Ketenimines for the Synthesis of Triazolopyrimidines

First simultaneous generation and utilization of both copper–triazole and −ketenimine intermediates in copper-catalyzed sulfonyl azide–alkyne cycloaddition reactions is achieved for the one-pot synthesis of triazolopyrimidines via a novel copper-catalyzed multicomponent cascade of sulfonyl azides, alkynes, and azirines. Significantly, the reaction proceeds under very mild conditions in good yields.本研究首次在铜催化磺酰叠氮-炔烃环加成反应中，实现了铜-三唑与烯酮亚胺两类中间体的同步生成与利用，并通过磺酰叠氮、炔烃及氮丙烯的新型铜催化多组分级联反应，成功实现了三唑并嘧啶类化合物的一锅法合成。值得注意的是，该反应可在极为温和的条件下以良好收率顺利进行。