Regioselective palladium-catalyzed synthesis of beta-arylated primary allylamine equivalents by an efficient Pd-N coordination

J Org Chem. 2001 Jan 26;66(2):544-9. doi: 10.1021/jo001416y.

Abstract

A highly regioselective Heck arylation, utilizing aryl triflates and a palladium/dppf catalytic system, can be performed at the internal, beta-carbon of Boc- and phthalimido-protected allylamines, yielding arylated primary allylamine equivalents. The very high regioselectivity obtained with secondary Boc-protected allylamides is suggested to be caused by an efficient coordination between an anionic nitrogen and palladium. Single-mode microwave irradiation has been utilized to shorten the reaction times and, in the case of Boc-protected allylamides, to improve the yields of two electron-poor aryl triflates.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Allylamine / analogs & derivatives*
  • Allylamine / chemical synthesis*
  • Allylamine / chemistry
  • Indicators and Reagents
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Molecular Structure
  • Palladium*
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Indicators and Reagents
  • Allylamine
  • Palladium