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Keywords:

  • Synthetic methods;
  • Heterocycles;
  • Fused-ring systems;
  • Homogeneous catalysis;
  • Palladium;
  • P ligands;
  • C–H functionalization

Abstract

The sequential imination and intramolecular palladium-catalyzed direct arylation of thiophene-3-carbaldehyde or furan-3-carbaldehyde with 2-haloanilines provided a one-pot access to furo- or thienoquinolines in high yields with H2O and HBr as the major waste. Both electron-withdrawing and -donating substituents on the 2-haloaniline derivatives were tolerated. These furo- or thienoquinoline derivatives can be employed in the direct arylation at C-5 of the furyl or thienyl moiety, and a variety of corresponding arylation products were obtained in high yields.