A transition-metal-free azide-alkyne cycloaddition / hydroamination cascade reaction for the construction of triazole-fused piperazin-2-ones

A time-dependent, divergent synthesis of highly functionalized [1,2,3]triazolo[1,5-a]pyrazin-4(5H)-one (reaction time: 12 h) or 6,7-dihydro-[1,2,3]triazolo[1,5-a]pyrazin-4(5H)-one (reaction time: 2 h) scaffolds via cascade azide-alkyne cycloaddition /hydroamination protocol is reported. The transformation features good functional group compatibility, broad substrate scope, high atom economy and avoiding the use of transition-metal catalysts.

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