Intermolecular C-H Aminocyanation of Indoles via Copper-iodine Cocatalyzed Tandem C-N/C-C Bond Formation

J Org Chem. 2022 Sep 16;87(18):12424-12433. doi: 10.1021/acs.joc.2c01703. Epub 2022 Aug 31.

Abstract

An efficient copper-iodine cocatalyzed intermolecular C-H aminocyanation of indoles with a broad substrate scope has been developed for the first time. This method enables highly step-economic access to 2-amino-3-cyanoindoles in moderate to good yields and provides a complementary strategy for the regioselective difunctionalization of carbon═carbon double bonds of interest in organic synthesis and related areas. Mechanistic studies suggest that these transformations are initiated by iodine-mediated C2-H amination with azoles, followed by copper-catalyzed C3-H cyanation with ethyl cyanoformate.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Azoles / chemistry
  • Catalysis
  • Copper / chemistry
  • Indoles* / chemistry
  • Iodides
  • Iodine* / chemistry

Substances

  • Azoles
  • Indoles
  • Iodides
  • Copper
  • Iodine