Synthesis of 1,4,2-Oxathiazoles via Oxidative Cyclization of Thiohydroximic Acids

Org Lett. 2015 Sep 18;17(18):4542-5. doi: 10.1021/acs.orglett.5b02256. Epub 2015 Sep 2.

Abstract

An oxidative formation of 1,4,2-oxathiazoles from readily available thiohydroximic acids is reported. A variety of alkyl, aryl, and heteroaryl substituents are well tolerated for both the thiohydroximic acid and activating fragments, and the reaction has been demonstrated on gram-scale. This reaction represents the only method currently available to prepare a diverse set of oxathiazoles and expands the chemistry of C-H oxidation via appended N-OH functional groups. Finally, we also demonstrate the rapid preparation of a 1,4,2-oxathiazole analog of an anticancer lead molecule.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Catalysis
  • Copper / chemistry
  • Cyclization
  • Molecular Structure
  • Oxidation-Reduction
  • Oximes / chemistry*
  • Thiazoles / chemical synthesis*
  • Thiazoles / chemistry

Substances

  • Antineoplastic Agents
  • Oximes
  • Thiazoles
  • thiohydroximic acid ester
  • Copper