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A facile and novel one-pot construction of diversely functionalized N-heteroaryl-2-pyridones is achieved by Cu(OTf)2-catalyzed [3+2+1] annulation of various 2-aminopyridines and β-enamino esters. The [3+2+1] annulation proceeds via domino two Michael additions/elimination/isomerization/intramolecular cyclization.

Graphical abstract: Novel construction of diversely functionalized N-heteroaryl-2-pyridones via copper(ii)-catalyzed [3+2+1] annulation

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