A divergent approach to 3-piperidinols: a concise syntheses of (+)-swainsonine and access to the 1-substituted quinolizidine skeleton

J Org Chem. 2012 Sep 21;77(18):7968-80. doi: 10.1021/jo3011914. Epub 2012 Aug 29.

Abstract

Nucleophilic addition of Grignard reagents and organolithium species to a 3-silyloxy-3,4,5,6-tetrahydropyridine N-oxide provides trans-2,3-disubstituted N-hydroxypiperidines exclusively. The application of this methodology to the preparation of a diversity of useful trans-2-substituted-3-hydroxypiperidines, a concise synthesis of (+)-swainsonine, and an enantiopure 1-substituted quinolizidine of utility in target-directed synthesis is reported.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Molecular Structure
  • Piperidines / chemistry*
  • Quinolizidines / chemistry*
  • Stereoisomerism
  • Swainsonine / chemical synthesis*
  • Swainsonine / chemistry

Substances

  • Piperidines
  • Quinolizidines
  • Swainsonine