Ring expansion of functionalized octahydroindoles to enantiopure cis-decahydroquinolines

J Org Chem. 2006 Aug 4;71(16):5930-5. doi: 10.1021/jo060592p.

Abstract

A new synthetic entry to enantiopure cis-decahydroquinolines is reported. Endo and exo derivatives of cis-1-benzyl-2-(hydroxymethyl)octahydroindol-6-one ethylene acetal undergo ring enlargement upon treatment with TFAA and then Et3N (thermodynamic conditions) to give enantiopure 1-benzyl-3-hydroxydecahydroquinolin-7-one derivatives in 77 and 82% yield, respectively. For 2-(1-hydroxyethyl) analogues, the best synthetic result is obtained from the (2S,1'R) endo isomer, which under kinetic reaction conditions (MsCl, THF, -20 degrees C, then AgOAc at rt ) gives the expanded product in 54% yield.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Hydrogen / chemistry*
  • Indoles / chemistry*
  • Kinetics
  • Methylation
  • Molecular Structure
  • Quinolines / chemical synthesis
  • Quinolines / chemistry*
  • Stereoisomerism
  • Thermodynamics

Substances

  • Indoles
  • Quinolines
  • Hydrogen
  • quinoline