Thio acid/azide amidation: an improved route to N-acyl sulfonamides

Org Lett. 2006 Mar 2;8(5):823-6. doi: 10.1021/ol052671d.

Abstract

A one-pot procedure for the conversion of carboxylic acids to N-acyl sulfonamides, via thio acid/azide amidation, is presented. The method is compatible with acid- and base-sensitive amino acid protection. N-Acyl sulfonamide synthesis on solid support, peptide thio acid/sulfonazide coupling, and N-alkyl amide synthesis via selective cleavage of sulfonyl from an N-alkyl-N-acyl sulfonamide are also reported.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemistry*
  • Amides / classification
  • Amino Acids / chemistry
  • Azides / chemistry*
  • Carboxylic Acids / chemistry*
  • Molecular Structure
  • Peptides / chemistry
  • Sulfonamides / chemical synthesis*
  • Sulfonamides / chemistry

Substances

  • Amides
  • Amino Acids
  • Azides
  • Carboxylic Acids
  • Peptides
  • Sulfonamides