摘要
Thesynthesis of chiral triazole-fused pyrazine scaffolds fromreadily available substrates in a step-economical asymmetric catalyticway is highly appealing. We herein report that an efficient Cu/Agrelay catalyzed protocol employing cascade asymmetric propargylicamination, hydroazidation, and [3 + 2] cycloaddition reaction withhigh efficiency to access the target enantioenriched 1,2,3-triazolo[1,5-a]pyrazine has been accomplished by applying a novel N,N,P-ligand. The one-potreaction of three components exhibits high functional group tolerance,excellent enantioselectivities, and a broad substrate scope with readilyavailable starting materials.