Access to functionalized 3H-pyrrolo[2,3-c]quinolin-4(5H)-ones and thieno[2,3-c]quinolin-4(5H)-ones via domino reaction of 4-alkynyl-3-bromoquinolin-2(1H)-ones

J Org Chem. 2014 Oct 17;79(20):9628-38. doi: 10.1021/jo501753p. Epub 2014 Oct 3.

Abstract

We describe two efficient protocols for the straightforward synthesis of 3H-pyrrolo[2,3-c]quinolin-4(5H)-one and thieno[2,3-c]quinolin-4(5H)-one derivatives from readily available 4-alkynyl-3-bromoquinolin-2(1H)-one as precursor. The efficient synthesis of highly functionalized 3H-pyrrolo[2,3-c]quinolin-4(5H)-ones has been achieved via a palladium-catalyzed domino reaction of 4-alkynyl-3-bromoquinolin-2(1H)-ones with amines. Thieno[2,3-c]quinolin-4(5H)-one derivatives were also conveniently synthesized via sequential nucleophilic aromatic substitution/5-endo-dig cyclization between 4-alkynyl-3-bromoquinolin-2(1H)-ones and sodium sulfide with good functional tolerance under mild conditions.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkynes / chemistry*
  • Catalysis
  • Molecular Structure
  • Palladium / chemistry
  • Pyrroles / chemical synthesis*
  • Pyrroles / chemistry*
  • Quinolones / chemical synthesis*
  • Quinolones / chemistry

Substances

  • 3H-pyrrolo(2,3-c)quinolin-4(5H)-one
  • Alkynes
  • Pyrroles
  • Quinolones
  • thieno(2,3-c)quinolin-4(5H)-one
  • Palladium