Telescoped Oxidation and Cycloaddition of Urazoles to Access Diazacyclobutenes

J Org Chem. 2022 Jun 3;87(11):7494-7500. doi: 10.1021/acs.joc.2c00280. Epub 2022 May 12.

Abstract

Our previous method to access the diazacyclobutene scaffold did not allow for modification of the substituent originating from the 1,2,4-triazoline-3,5-dione component. We have circumvented this challenge and expanded access to additional structural diversity of the scaffold. A telescoped urazole oxidation and Lewis acid-catalyzed cyclization provided R3-substituted diazacyclobutenes. Calcium hypochlorite-mediated oxidation of urazoles followed by MgCl2-catalyzed cyclization of the resulting triazolinediones with thioalkynes promoted the formation of diazacyclobutenes bearing substitution at the R3 position originating from the triazolinedione component.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cyclization
  • Cycloaddition Reaction
  • Molecular Structure
  • Triazoles* / chemistry

Substances

  • Triazoles
  • urazole