Cu/Ag-Mediated One-Pot Enantioselective Synthesis of Fully Decorated 1,2,3-Triazolo[1,5-a]pyrazines

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.

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