Iodine-mediated solvent-controlled selective electrophilic cyclization and oxidative esterification of o-alkynyl aldehydes: an easy access to pyranoquinolines, pyranoquinolinones, and isocumarins

J Org Chem. 2010 Nov 19;75(22):7691-703. doi: 10.1021/jo101526b. Epub 2010 Oct 29.

Abstract

Chemoselective behavior of iodine in different solvents in the electrophilic iodocyclization of o-alkynyl aldehydes is described. o-Alkynyl aldehydes 3a-t on reaction with I2 in CH2Cl2 with appropriate nucleophiles provides pyrano[4,3-b]quinolines 4a-f, via formation of cyclic iodonium intermediate Q; however, using alcohols as a solvent as well as nucleophile, o-alkynyl esters 5a-y were obtained selectively in good to excellent yields via formation of hypoiodide intermediate R. Subsequently, o-alkynyl esters were converted in to pyranoquinolinones 6a-i and isocoumarin 6j by electrophilic iodocyclization. This developed oxidative esterification provides a novel access for the chemoselective synthesis of esters 5q-u from aldehydes 3n-p without oxidizing primary alcohol present in the substrate.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aldehydes / chemistry*
  • Alkynes / chemistry*
  • Catalysis
  • Cyclization
  • Esterification
  • Iodine / chemistry*
  • Isocoumarins / chemical synthesis*
  • Isocoumarins / chemistry
  • Molecular Structure
  • Oxidation-Reduction
  • Quinolines / chemical synthesis*
  • Quinolines / chemistry
  • Solvents / chemistry*

Substances

  • Aldehydes
  • Alkynes
  • Isocoumarins
  • Quinolines
  • Solvents
  • Iodine