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Updated: Aug 24, 2026

A Microwave-Assisted Direct Heteroarylation of Ketones Using Transition Metal Catalysis
Published on: February 16, 2020
Native Amine-Directed NiH-Catalyzed Markovnikov Hydroalkynylation of Unactivated Alkenes
Lu Yang1, Yunzheng Wang1, Rui He1
1Tianjin Key Laboratory of Structure and Performance for Functional Molecules; College of Chemistry, Tianjin Normal University, Tianjin300387, P. R. China.
Abstract:
The native amine-directed hydroalkynylation of unactivated alkenes remains a significant challenge because of the strong coordination ability of free amines and the difficulty in controlling regioselectivity during alkene functionalization. Herein, we report a NiH-catalyzed Markovnikov-selective hydroalkynylation of unactivated alkenes enabled by a diamine-based ligand. This operationally simple protocol provides efficient access to structurally diverse β-, γ- and δ-aminoalkynes from readily available alkenyl amines and alkynyl bromides under mild conditions. The practicality of this method is further demonstrated through gram-scale synthesis and late-stage functionalization of pharmaceutically relevant molecules.
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