Modular Access to Arylethylamines Enabled by Ni‐Catalyzed Markovnikov ‐Selective Hydroarylation of Allylic Amines

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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.
Funding Information
  • National Key Research and Development Program of China (2021YFF0701600)
  • National Natural Science Foundation of China (22325110)
  • National Natural Science Foundation of China (92256303)
  • National Natural Science Foundation of China (22171280)
  • National Natural Science Foundation of China (22401288)
  • Program of Shanghai Academic Research Leader (22XD1424900)
  • Science and Technology Commission of Shanghai Municipality (24ZR1479000)
  • Natural Science Foundation of Ningbo Municipality (2022J017)

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