Modular Access to Arylethylamines Enabled by Ni‐Catalyzed <i>Markovnikov</i> ‐Selective Hydroarylation of Allylic Amines

H Hai‐Yu Wu (State 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) M Ming Joo Koh Z Zi‐Chao Wang (State 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) S Shi‐Liang Shi (State 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

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.

Article Details

Volume / Issue Vol. 64, Issue 28
Published July 07, 2025
ISSN 1433-7851
Publisher Wiley

Journal Info

Angewandte Chemie International Edition

Wiley

ISSN: 1433-7851 Physical Sciences

Authors (4)

H

Hai‐Yu Wu

State 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

M

Ming Joo Koh

Z

Zi‐Chao Wang

State 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

S

Shi‐Liang Shi

State 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