Alkylation of Sulfonamides with Trichloroacetimidates under Thermal Conditions

J Org Chem. 2016 Sep 2;81(17):8035-42. doi: 10.1021/acs.joc.6b01421. Epub 2016 Aug 10.

Abstract

An intermolecular alkylation of sulfonamides with trichloroacetimidates is reported. This transformation does not require an exogenous acid, base, or transition metal catalyst; instead the addition occurs in refluxing toluene without additives. The sulfonamide alkylation partner appears to be only limited by sterics, with unsubstituted sulfonamides providing better yields than more encumbered N-alkyl sulfonamides. The trichloroacetimidate alkylating agent must be a stable cation precursor for the substitution reaction to proceed under these conditions.

Publication types

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

MeSH terms

  • Acetamides / chemistry*
  • Alkylation
  • Carbon-13 Magnetic Resonance Spectroscopy
  • Chloroacetates / chemistry*
  • Chromatography, High Pressure Liquid
  • Proton Magnetic Resonance Spectroscopy
  • Sulfonamides / chemistry*
  • Temperature

Substances

  • Acetamides
  • Chloroacetates
  • Sulfonamides
  • trichloroacetamide