Nine-step enantioselective total synthesis of (-)-vincorine

J Am Chem Soc. 2013 May 1;135(17):6442-5. doi: 10.1021/ja402933s. Epub 2013 Apr 19.

Abstract

A concise and highly enantioselective total synthesis of the akuammiline alkaloid (-)-vincorine has been accomplished. A key element of the synthesis is a stereoselective organocatalytic Diels-Alder, iminium cyclization cascade sequence, which serves to construct the tetracyclic alkaloid core architecture in one step from simple achiral precursors. The challenging seven-membered azepanyl ring system is installed by way of a single electron-mediated cyclization event initiated from an acyl telluride precursor. The total synthesis of (-)-vincorine is achieved in nine steps and 9% overall yield from commercially available starting materials.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cyclization
  • Indicators and Reagents
  • Magnetic Resonance Spectroscopy
  • Models, Molecular
  • Stereoisomerism
  • Vinca Alkaloids / chemical synthesis*
  • Vinca Alkaloids / chemistry
  • X-Ray Diffraction

Substances

  • Indicators and Reagents
  • Vinca Alkaloids
  • vincorine