Copper-Promoted N-Alkylation and Bromination of Arylamines/Indazoles Using Alkyl Bromides as Reagents for Difunctionalization

J Org Chem. 2022 Sep 16;87(18):12214-12224. doi: 10.1021/acs.joc.2c01356. Epub 2022 Sep 2.

Abstract

Practical copper-promoted N-alkylation and bromination of arylamines/indazoles with alkyl bromides are described; the N-alkylation-C-4-bromination and N-dialkylation-C-4-bromination of arylamines, and N-alkylation-C-3-bromination of indazoles, with alkyl bromides have been analyzed. The full use of alkyl bromides as alkylating and brominating building blocks without atom wastage, indicating excellent atom and step economy, has been highlighted. Eco-friendly oxygen and water are the reaction oxidant and byproduct, respectively.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Amines
  • Bromides*
  • Copper*
  • Halogenation
  • Indazoles
  • Indicators and Reagents
  • Oxidants
  • Oxygen
  • Water

Substances

  • Amines
  • Bromides
  • Indazoles
  • Indicators and Reagents
  • Oxidants
  • Water
  • Copper
  • Oxygen