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A copper-catalyzed coupling-cyclization reaction of N-acyl enamides with electron-deficient alkynes is developed. This reaction tolerates a wide range of N-acyl enamines and provides a simple and efficient method for the synthesis of 3-alkynyl-substituted pyridines in good to high yields from easily available acyclic starting materials with only water and hydrogen as the by-products in a single step.

Graphical abstract: A copper-catalyzed tandem cyclization reaction of N-acyl enamines and electron-deficient alkynes: direct synthesis of alkynyl substituted pyridines

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