Kinetic resolution of 2-substituted 2,3-dihydro-4-pyridones by palladium-catalyzed asymmetric allylic alkylation: catalytic asymmetric total synthesis of indolizidine (-)-209I

Org Lett. 2014 Apr 4;16(7):1944-7. doi: 10.1021/ol500498m. Epub 2014 Mar 24.

Abstract

The kinetic resolution of 2-substituted-2,3-dihydro-4-pyridones was realized via a Pd-catalyzed allylic substitution reaction using a commercially available (S)-P-Phos as a ligand, affording optically active dihydropyridones and C-allylated dihydropyridones in high yields and good enantioselectivities with the S-factor up to 43. With this protocol, a catalytic asymmetric total synthesis of indolizidine (-)-209I was realized for the first time.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / chemical synthesis*
  • Alkaloids / chemistry
  • Alkylation
  • Animals
  • Catalysis
  • Combinatorial Chemistry Techniques
  • Indolizidines / chemical synthesis*
  • Indolizidines / chemistry
  • Kinetics
  • Molecular Structure
  • Palladium / chemistry*
  • Pyridones / chemistry*
  • Ranidae
  • Skin / chemistry
  • Stereoisomerism

Substances

  • Alkaloids
  • Indolizidines
  • Pyridones
  • indolizidine 209I
  • Palladium