Abstract
The Michael addition and three-component cyclization reaction of amines, alkynes and dialkyl acetylene dicarboxylates to form pyridones has been developed. Aliphatic amines and aromatic amines could selectively be converted into N-alkyl-disubstituted 2-pyridones and N-aryl-trisubstituted 2-pyridones with good yields in the presence of wet ethanol, which means a suitable amount of water is required for this reaction. The Michael addition and cyclization reaction process was confirmed through deuterium-labeling experiments, intermediates isolation and control experiments.
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