Sequential and one-pot reactions of phenols with bromoalkynes for the synthesis of (Z)-2-bromovinyl phenyl ethers and benzo[b]furans

Org Lett. 2011 Nov 18;13(22):5968-71. doi: 10.1021/ol202383z. Epub 2011 Oct 18.

Abstract

Benzo[b]furans were prepared in one pot based on the addition/palladium-catalyzed C-H bond functionalization of phenols with bromoalkynes. The addition reactions of phenols to bromoalkynes generated (Z)-2-bromovinyl phenyl ethers in high yields with excellent regio- and stereoselectivity. The obtained (Z)-2-bromovinyl phenyl ethers subsequently proceeded by intramolecular cyclization to afford 2-substituted benzo[b]furans in good yields through palladium-catalyzed direct C-H bond functionalizations. It is important to note that the transformation of phenols with bromoalkynes into benzo[b]furans could be carried out in one pot with a simple and efficient tandem procedure.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkynes / chemistry*
  • Benzofurans / chemical synthesis*
  • Bromine / chemistry*
  • Cyclization
  • Molecular Structure
  • Palladium / chemistry
  • Phenols / chemistry*
  • Phenyl Ethers / chemical synthesis*
  • Vinyl Compounds / chemical synthesis*

Substances

  • Alkynes
  • Benzofurans
  • Phenols
  • Phenyl Ethers
  • Vinyl Compounds
  • Palladium
  • phenyl vinyl ether
  • Bromine