Application of secondary alkyl halides to a domino aryl alkylation reaction for the synthesis of aromatic heterocycles

J Org Chem. 2009 Jan 2;74(1):289-97. doi: 10.1021/jo802180h.

Abstract

A palladium-catalyzed, norbornene-mediated ortho-alkylation reaction of aryl iodides with secondary alkyl halides is described. Intermolecular or intramolecular ortho-alkylation proceeds in a domino process with various termination steps, generating two new carbon-carbon or carbon-nitrogen bonds in one pot, to afford an array of polycyclic heterocycles. The use of enantioenriched substrates has shown that this palladium-catalyzed reaction is stereospecific, proceeding with minimal erosion of ee.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Catalysis
  • Heterocyclic Compounds / chemical synthesis*
  • Heterocyclic Compounds / chemistry
  • Hydrocarbons, Halogenated / chemistry*
  • Molecular Structure
  • Norbornanes / chemistry
  • Palladium / chemistry
  • Polycyclic Aromatic Hydrocarbons / chemical synthesis*
  • Polycyclic Aromatic Hydrocarbons / chemistry
  • Stereoisomerism

Substances

  • Heterocyclic Compounds
  • Hydrocarbons, Halogenated
  • Norbornanes
  • Polycyclic Aromatic Hydrocarbons
  • Palladium