Synthesis of substituted tetrahydroindoloisoquinoline derivatives via intramolecular Pd-catalyzed alkene carboamination reactions

J Org Chem. 2014 May 2;79(9):4212-7. doi: 10.1021/jo500470m. Epub 2014 Apr 11.

Abstract

Intramolecular Pd-catalyzed alkene carboamination reactions of substituted 2-allyl-N-(2-bromobenzyl)anilines are described. The substrates for these reactions are generated in two steps from readily available 2-allylanilines and 2-bromobenzaldehyde derivatives. The transformations afford substituted tetrahydroindoloisoquinolines, an uncommon class of fused bicyclic heterocycles, in good yield. The mechanism of these transformations is described, and a model that accounts for the observed product stereochemistry is proposed.

Publication types

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

MeSH terms

  • Alkenes / chemistry*
  • Amination
  • Catalysis
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Isoquinolines / chemical synthesis*
  • Isoquinolines / chemistry
  • Molecular Structure
  • Palladium / chemistry*

Substances

  • Alkenes
  • Indoles
  • Isoquinolines
  • Palladium