Metal-Free Regioselective N2-Arylation of 1 H-Tetrazoles with Diaryliodonium Salts

J Org Chem. 2022 Aug 5;87(15):9782-9796. doi: 10.1021/acs.joc.2c00848. Epub 2022 Jul 18.

Abstract

We describe a simple, metal-free regioselective N2-arylation strategy for 5-substituted-1H-tetrazoles with diaryliodonium salts to access 2-aryl-5-substituted-tetrazoles. Diaryliodonium salts with a wide range of both electron-rich and previously challenged electron-deficient aryl groups are applicable in this method. Diversely functionalized tetrazoles are tolerable also. We have devised a one-pot system to synthesize 2,5-diaryl-tetrazoles directly from nitriles. The synthetic utility of this method is furthered extended to late-stage arylation of two biologically active molecules.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Metals
  • Molecular Structure
  • Onium Compounds*
  • Salts*
  • Tetrazoles

Substances

  • Metals
  • Onium Compounds
  • Salts
  • Tetrazoles
  • 1H-tetrazole