Copper-Catalyzed Aminoheteroarylation of Unactivated Alkenes through Distal Heteroaryl Migration

Journal Article (Journal Article)

We report a copper-catalyzed aminoheteroarylation of unactivated alkenes to access valuable heteroarylethylamine motif. The developed reaction features a copper-catalyzed intermolecular electrophilic amination of the alkenes followed by a migratory heteroarylation. The method applies to alcohol-, amide-, and ether-containing alkenes, overcoming the common requirement of a hydroxyl motif in previous migratory difunctionalization reactions. This reaction is effective for the introduction of diverse aliphatic amines and has good functional group tolerance, which is particularly useful for rich functionalized heteroarenes. This migration-involved reaction was found well suited as a powerful ring-expansion approach for the construction of medium-sized rings that are in great demand in medicinal chemistry.

Full Text

Duke Authors

Cited Authors

  • Kwon, Y; Zhang, W; Wang, Q

Published Date

  • July 16, 2021

Published In

Volume / Issue

  • 11 / 14

Start / End Page

  • 8807 - 8817

Electronic International Standard Serial Number (EISSN)

  • 2155-5435

Digital Object Identifier (DOI)

  • 10.1021/acscatal.1c01001

Citation Source

  • Scopus