Double conjugate addition of dithiols to propargylic carbonyl systems to generate protected 1,3-dicarbonyl compounds

J Org Chem. 2006 Mar 31;71(7):2715-25. doi: 10.1021/jo052514s.

Abstract

The work describes the efficient double conjugate addition of ethane and propane dithiols in the presence of sodium methoxide to a wide variety of propargylic carbonyl containing compounds. The products of these reactions are differentiated, 1,3-dicarbonyl systems useful for various synthesis programs. By judicious use of hydroxylated substrates tandem cyclization occurs to afford tetrahydropyran lactols or, in the case of hydroxy-substituted propargylic esters, lactones. The corresponding amino-substituted propargylic aldehydes gives piperidine derivatives upon double conjugate addition tandem cyclization.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aldehydes / chemistry*
  • Cyclization
  • Molecular Structure
  • Piperidines / chemical synthesis*
  • Piperidines / chemistry
  • Stereoisomerism
  • Sulfhydryl Compounds / chemistry*

Substances

  • Aldehydes
  • Piperidines
  • Sulfhydryl Compounds