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Updated: May 12, 2025

A Microwave-Assisted Direct Heteroarylation of Ketones Using Transition Metal Catalysis
Published on: February 16, 2020
Modular Access to Arylethylamines Enabled by Ni-Catalyzed Markovnikov-Selective Hydroarylation of Allylic Amines
Hai-Yu Wu1, Ming Joo Koh2, Zi-Chao Wang1
1State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032, P.R. China.
Abstract:
Arylethylamines are prevalent structural skeletons in bioactive molecules and have significant interest within the organic chemistry community. We report here a modular and efficient nickel-catalyzed Markovnikov-selective hydroarylation of readily available allylic amines, delivering a wide variety of valuable arylethylamines with complete regiocontrol under mild conditions. Key to the success of this protocol is the employment of bulky N-heterocyclic carbenes (NHCs) as ligands. Furthermore, the use of chiral NHC ligands enables straightforward access to enantioenriched arylethylamines with excellent regio- and enantioselectivities.
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