Redox-neutral α-sulfenylation of secondary amines: ring-fused N,S-acetals

Org Lett. 2014 Jul 3;16(13):3556-9. doi: 10.1021/ol501509b. Epub 2014 Jun 13.

Abstract

Secondary amines react with thiosalicylaldehydes in the presence of catalytic amounts of acetic acid to generate ring-fused N,S-acetals in redox-neutral fashion. A broad range of amines undergo α-sulfenylation, including challenging substrates such morpholine, thiomorpholine, and piperazines. Computational studies employing density functional theory indicate that acetic acid reduces the energy barriers of two separate steps, both of which involve proton transfer.

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

  • Acetals / chemical synthesis*
  • Acetals / chemistry
  • Acetic Acid / chemistry
  • Amines / chemistry*
  • Catalysis
  • Molecular Structure
  • Morpholines / chemistry
  • Oxidation-Reduction
  • Piperazines / chemistry
  • Protons

Substances

  • Acetals
  • Amines
  • Morpholines
  • Piperazines
  • Protons
  • thiamorpholine
  • morpholine
  • Acetic Acid