Regioselective Formal Hydroamidation of Alkynes: Synthesis of α‐Substituted Acrylamides

Abstract

The formal hydroamidation of alkyne is a powerful synthetic method that enables the formation of various α,β‐unsaturated amides. In this article, the efficient formal hydroamidation of terminal and internal alkynes is described, which constitutes the Ni‐catalyzed α‐selective hydroalumination of alkynes and subsequent treatment with isocyanates. This method is gram‐scalable and the synthetic utility is highlighted by the synthesis of a β‐lactam from α‐phenyl acrylamide.