Development and Utilization of a Palladium-Catalyzed Dehydration of Primary Amides To Form Nitriles

Org Lett. 2018 Oct 5;20(19):6046-6050. doi: 10.1021/acs.orglett.8b02422. Epub 2018 Sep 17.

Abstract

A palladium(II) catalyst, in the presence of Selectfluor, enables the efficient and chemoselective transformation of primary amides into nitriles. The amides can be attached to aromatic rings, heteroaromatic rings, or aliphatic side chains, and the reactions tolerate steric bulk and electronic modification. Dehydration of a peptaibol containing three glutamine groups afforded structure-activity relationships for each glutamine residue. Thus, this dehydration can act similarly to an alanine scan for glutamines via synthetic mutation.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Amides / chemistry*
  • Catalysis
  • Nitriles / chemistry*
  • Palladium / chemistry*
  • Water / chemistry

Substances

  • Amides
  • Nitriles
  • Water
  • Palladium