Development of a bio-inspired acyl-anion equivalent macrocyclization and synthesis of a trans-resorcylide precursor

J Org Chem. 2007 Jul 6;72(14):5260-9. doi: 10.1021/jo070676d. Epub 2007 Jun 19.

Abstract

Studies on the macrocyclization of alpha,omega-dialdehydes have revealed a strong dependence on ring size with respect to the ultimate efficiency of the reaction. Strong catalyst dependence was observed, as thiazolium salts led to no detectable product formation, whereas electron-deficient triazolium salts served as precatalysts for the cyclization. Surprisingly, the N-pentafluorophenyl triazolium variant led to cyclization at room temperature within a short 90-min reaction time. These findings were applied to a range of substrates, including the synthesis of a key intermediate in a rapid synthesis of trans-resorcylide.

Publication types

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

MeSH terms

  • Acylation
  • Aldehydes / chemistry
  • Anions / chemistry*
  • Crystallography, X-Ray
  • Cyclization
  • Electrons
  • Isomerism
  • Ketones / chemistry
  • Macrolides / chemistry*
  • Models, Molecular
  • Molecular Structure

Substances

  • Aldehydes
  • Anions
  • Ketones
  • Macrolides