The
synthesis of chiral triazole-fused pyrazine scaffolds from
readily available substrates in a step-economical asymmetric catalytic
way is highly appealing. We herein report that an efficient Cu/Ag
relay catalyzed protocol employing cascade asymmetric propargylic
amination, hydroazidation, and [3 + 2] cycloaddition reaction with
high 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-pot
reaction of three components exhibits high functional group tolerance,
excellent enantioselectivities, and a broad substrate scope with readily
available starting materials.