NDTP Mediated Direct Rapid Amide and Peptide Synthesis without Epimerization

Org Lett. 2022 Feb 11;24(5):1169-1174. doi: 10.1021/acs.orglett.1c04258. Epub 2022 Jan 7.

Abstract

Herein, we explored an unprecedented mild, nonirritating, conveniently available, and recyclable coupling reagent NDTP, which could activate the carboxylic acids via acyl thiocyanide and enable the rapid amide and peptide synthesis at very mild conditions. In addition, the methodology was compatible with Fmoc-SPPS, which may provide an alternative to peptide manufacturing.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemical synthesis*
  • Amides / chemistry
  • Carboxylic Acids / chemistry
  • Molecular Structure
  • Peptides / chemical synthesis*
  • Peptides / chemistry
  • Stereoisomerism
  • Thiocyanates / chemistry

Substances

  • Amides
  • Carboxylic Acids
  • Peptides
  • Thiocyanates
  • thiocyanate