Metal‐catalyzed azide‐alkyne cycloaddition reactions represent the most convenient and atom‐economic way to construct robust 1,2,3‐triazole units. Remarkable copper‐ and ruthenium‐based catalytic systems have been well established for regioselective preparation of 1,4‐ and 1,5‐disubstituted 1,2,3‐triazoles, both of which have been widely utilized in various areas. In comparison, exploitation of efficient methods to promote the cycloaddition of azides with internal alkynes to afford 1,4,5‐trisubstituted 1,2,3‐triazole motifs with high regioselectivity is still challenging and attractive. This review provides a thorough summary of the developments in metal‐catalyzed cycloaddition of azides with internal alkynes. Besides discussions about mechanism and scope, applications of these strategies were also briefly overviewed.

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过渡金属催化的叠氮化物与内部炔烃的环加成反应

金属催化的叠氮化物-炔烃环加成反应是构建坚固的1,2,3-三唑单元的最便捷，最经济的方法。良好的基于​​铜和钌的催化体系已经很好地用于区域选择性制备1,4-和1,5-二取代的1,2,3-三唑，这两种催化剂已广泛应用于各个领域。相比之下，开发有效的方法以促进叠氮化合物与内部炔烃的环加成反应以提供具有高区域选择性的1,4,5-三取代的1,2,3-三唑基序仍然具有挑战性和吸引力。这篇综述详尽地总结了叠氮化物与内部炔烃在金属催化的环加成反应中的发展。除了讨论机制和范围外，还简要概述了这些策略的应用。