Abstract

A domino catalytic reaction between terminal alkynes, isocyanates, and malonates has been developed. Copper acetylides attack on isocyanates to form a propargylic amide species which further reacted with malonates by the action of t-BuOLi to form dihydropyridine-3-carboxylates. The regioselectivity of the reaction has been examined with unsymmetrical malonate. The procedure is easy to implement, has a broad scope and allows the construction of the scaffolds by creating three covalent bonds in one pot.

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