Synthesis of (-)-tetrodotoxin: preparation of an advanced cyclohexenone intermediate

J Org Chem. 2003 Oct 3;68(20):7768-71. doi: 10.1021/jo0301189.

Abstract

The preparation of an advanced intermediate toward the enantioselective synthesis of tetrodotoxin is outlined. The enantiomerically pure cyclopentene 15 was generated from ketone 14 by alkylidene carbene insertion with retention of absolute configuration. An ozonolysis/aldol sequence first produced the trans cyclohexenone, which upon epimerization gave the more stable cis enone 18.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Cyclohexanones / chemical synthesis*
  • Hydrocarbons
  • Methane / analogs & derivatives*
  • Methane / chemistry
  • Ozone / chemistry
  • Stereoisomerism
  • Tetrodotoxin / chemical synthesis*
  • Tetrodotoxin / chemistry

Substances

  • Cyclohexanones
  • Hydrocarbons
  • carbene
  • Tetrodotoxin
  • Ozone
  • Methane