Zinc-catalyzed reactions of ethenetricarboxylates with 2-(trimethylsilylethynyl)anilines leading to bridged quinoline derivatives

Org Lett. 2009 Jul 2;11(13):2796-9. doi: 10.1021/ol900960q.

Abstract

Zinc Lewis acid-catalyzed cyclization of ethenetricarboxylate derivatives 1 with 2-ethynylanilines has been examined. Reaction of 1,1-diethyl 2-tert-butyl ethenetricarboxylate 1b with 2-(trimethylsilylethynyl)aniline substrates in the presence of Zn(OTf)(2) gave bridged quinoline derivatives in 43-85% yield. The reaction of 1b with 2'-aminoacetophenone also gave the bridged quinoline derivative in 41% yield. Thermal reaction of bridged quinolines (180-190 degrees C) afforded indole derivatives in moderate to good yields.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aniline Compounds / chemistry*
  • Catalysis
  • Heterocyclic Compounds, Bridged-Ring / chemical synthesis*
  • Heterocyclic Compounds, Bridged-Ring / chemistry
  • Indoles / chemical synthesis
  • Indoles / chemistry
  • Molecular Structure
  • Quinolines / chemical synthesis*
  • Quinolines / chemistry
  • Tricarboxylic Acids / chemistry*
  • Zinc / chemistry*

Substances

  • Aniline Compounds
  • Heterocyclic Compounds, Bridged-Ring
  • Indoles
  • Quinolines
  • Tricarboxylic Acids
  • Zinc