Cs₂CO₃‐Catalyzed Multi‐Component One‐Pot Stepwise Route for the Synthesis of Polysubstituted 2‐Pyridones

Abstract

A concise and practicable route to the synthesis of multisubstituted 2‐pyridones via a four‐component one‐pot stepwise cyclization catalyzed by Cs2CO3 has been developed. During this stepwise transformation, two new C‐C bonds and two new C‐N bonds were generated through an intermolecular condensation/aza‐Michael reaction/intermolecular Michael addition/intramolecular cyclization sequence. The alternative protocol offers a complementary route to provide a series of structurally diverse polysubstituted 2‐pyridones (21 examples) in good to excellent yields (52–81%) from easily available raw materials arylamines, dialkyl acetylenedicarboxylate, 1,3‐dicarbonyl compounds, and trialkyl orthoformate under mild conditions. It might provide new opportunities for the discovery of 2‐pyridones‐containing drugs.