Abstract
Herein, we report an efficient 1,5,7-Triazabicyclo[4.4.0]dec-5-ene (TBD)-catalyzed tandem intermolecular amidation and regioselective intramolecular 6-exo-dig cyclization of alkynyl esters to efficiently access pyrazine-1(2H)-one scaffolds. This organo-catalyzed [5 + 1] annulation features a broad substrate scope concerning both annulating partners. Total syntheses of peramine and formal syntheses of dibromophakellin natural products were achieved to show the application potential of the method.
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