The first aza Diels-Alder reaction involving an alpha,beta-unsaturated hydrazone as the dienophile: stereoselective synthesis of C-4 functionalized 1,2,3,4-tetrahydroquinolines containing a quaternary stereocenter

Org Biomol Chem. 2007 May 7;5(9):1351-3. doi: 10.1039/b703083e. Epub 2007 Apr 4.

Abstract

The reaction between aromatic imines and methacrolein dimethylhydrazone in the presence of 10% indium trichloride affords in good to excellent yields biologically and synthetically relevant 1,2,3,4-tetrahydroquinolines bearing a hydrazone function at C-4 in a one-pot process that involves the formation of two C-C bonds and the stereoselective generation of two stereocenters, one of them quaternary, and this constitutes the first example of an alpha,beta-unsaturated dimethylhydrazone behaving as a dienophile in a hetero Diels-Alder reaction and the first vinylogous aza-Povarov reaction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aldehydes / chemistry
  • Aniline Compounds / chemistry
  • Catalysis
  • Hydrazones / chemical synthesis*
  • Hydrazones / chemistry*
  • Quinolines / chemical synthesis*
  • Quinolines / chemistry*
  • Stereoisomerism

Substances

  • Aldehydes
  • Aniline Compounds
  • Hydrazones
  • Quinolines
  • aniline