Substituent-controlled Chemoselective Synthesis of Multi-substituted Pyridones via One-pot Three-component Cascade Reaction
An efficient and concise one-pot strategy for the synthesis of multisubstituted pyridones via one-pot three-component cascade reaction catalyzed by Cs2CO3 under solvent-free conditions has been developed. The substituent-controlled chemoselective cycloaddition process involved steps including a Michael addition/ethanol elimination/intermolecular cyclization sequence by utilizing anilines, diethyl acetylenedicarboxylate,and diethyl ethoxymethylenemalonate. In doing so, various 2-pyridone and 4-pyridone species (41 examples) could be obtained in good to excellent yields.
- This article is part of the themed collection: Synthetic methodology in OBC