Open-Air Dual-Diamination of Aromatic Aldehydes: Direct Synthesis of Azolo-Fused 1,3,5-Triazines Facilitated by Ammonium Iodide

J Org Chem. 2021 Dec 3;86(23):17265-17273. doi: 10.1021/acs.joc.1c02362. Epub 2021 Nov 18.

Abstract

A new and practical protocol for the synthesis of medicinally privileged azolo[1,3,5]triazines by simply heating under air has been presented. The in situ generated N-azolo amidines from commercially available aromatic aldehydes and 3-aminoazoles with ammonium iodide undergo the second diamination to accomplish the [3 + 1 + 1 + 1] heteroannulation reaction. This convenient process is appreciated by high efficiency, broad substrate scope, gram-scale synthesis, and operational simplicity under reagent-free conditions.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aldehydes*
  • Amidines
  • Ammonium Compounds
  • Indicators and Reagents
  • Triazines*

Substances

  • Aldehydes
  • Amidines
  • Ammonium Compounds
  • Indicators and Reagents
  • Triazines
  • ammonium iodide