I2/O2-Enabled N-S Bond Formation to Access Functionalized 1,2,3-Thiadiazoles

Org Lett. 2016 Mar 18;18(6):1258-61. doi: 10.1021/acs.orglett.6b00079. Epub 2016 Mar 1.

Abstract

A new, metal-free intermolecular formal [3 + 2] heterocyclization between triethylammonium thiolates and aryl hydrazines has been established by using the combination of I2 and O2 as efficient oxidation sources, allowing a concise and low-cost access to new densely functionalized 1,2,3-thiadiazoles with good to excellent yields. The reaction showed a broad scope of substrates of both reactants and attractive characteristics consisting of eco-friendly oxidants, flexible structural modification, broad functional group compatibility, and mild reaction conditions.

Publication types

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

MeSH terms

  • Catalysis
  • Hydrazines / chemistry*
  • Molecular Structure
  • Oxidants / chemistry
  • Oxidation-Reduction
  • Thiadiazoles / chemical synthesis*
  • Thiadiazoles / chemistry

Substances

  • Hydrazines
  • Oxidants
  • Thiadiazoles