Copper-catalyzed oxidative annulation between 2-aminopyridine and arylidenemalononitrile leading to 4-oxo-pyrido[1,2-a]pyrimidine-3-carbonitrile

A new strategy has been developed for the synthesis of 4-oxo-pyrido[1,2-a]pyrimidine-3-carbonitriles through Cu(I)-catalyzed annulation between 2-aminopyridine and arylidenemalononitriles under oxygen atmosphere. The transformation occurs through mechanistically different steps of aza-Michael addition, aerobic dehydrogenation, and intramolecular amidination followed by hydrolysis under Cu-catalysis.

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