Nickel-Catalyzed Hydroamination of Olefins with Anthranils

J Org Chem. 2021 Sep 3;86(17):12107-12118. doi: 10.1021/acs.joc.1c01430. Epub 2021 Aug 24.

Abstract

A nickel-catalyzed polarity-reversed hydroamination of olefins has been achieved with anthranils as the electrophilic aminating agents and hydrosilane as the reductant. This protocol provides a facile access to N-alkyl-2-aminobenzophenones that are versatile intermediates in organic synthesis. A wide range of olefins and anthranils are compatible in this transformation, delivering the desired amines in useful to excellent yields (38 examples, up to 92% yield). The utility of this protocol is exhibited in the late-stage functionalization of drug molecules and the valuable derivatives of the obtained amination products.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkenes*
  • Amination
  • Catalysis
  • Copper
  • Isoxazoles
  • Nickel*

Substances

  • Alkenes
  • Isoxazoles
  • anthranil
  • Copper
  • Nickel