Electro-Oxidative C-N Bond Formation through Azolation of Indole Derivatives: An Access to 3-Substituent-2-(Azol-1-yl)indoles

J Org Chem. 2021 Nov 19;86(22):16059-16067. doi: 10.1021/acs.joc.1c01271. Epub 2021 Sep 14.

Abstract

A practical protocol to synthesize 3-substituent-2-(azol-1-yl)indole derivatives has been developed via an electrochemical oxidative cross coupling process under mild conditions. This electro-oxidative C-N bond formation strategy tolerates a range of functional groups and is amenable to gram scale synthesis. Moreover, this method was applied to the late-stage functionalization of bioactive molecules.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Danazol*
  • Indoles*
  • Molecular Structure
  • Oxidative Stress

Substances

  • 2-(azol-1-yl)indole
  • Indoles
  • Danazol