Abstract

A convenient and novel 1,3-dimethylbarbituric acid-mediated methodology for constructing diverse benzimidazole-fused heteroaromatics has been developed. This metal-free cascade annulation of readily available 3-formylchromones, 1,2-diaminoarenes, and cyclic 1,3-dicarbonyl compounds provides an alternative synthetic route in the green conditions. 1,3-Dimethylbarbituric acid acts as a protecting group and accelerates intramolecular cyclization. This one-pot protocol proceeds through cascade nucleophilic addition, ring-opening, Michael-type addition, intramolecular cyclization, elimination, and air oxidation reactions.

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