Lewis Acid Catalyzed Displacement of Trichloroacetimidates in the Synthesis of Functionalized Pyrroloindolines

Org Lett. 2016 Aug 19;18(16):4100-3. doi: 10.1021/acs.orglett.6b02024. Epub 2016 Aug 3.

Abstract

The pyrroloindoline core is found in many natural products. These structures often differ at the C3a position, which may be substituted with an oxygen, nitrogen, or sp(3)- or sp(2)-hybridized carbon. Utilizing a trichloroacetimidate leaving group, a diversity-oriented approach to these structures has been developed. The trichloroacetimidate intermediate allows for the rapid incorporation of anilines, alcohols, thiols, and carbon nucleophiles. This method was applied in the synthesis of arundinine and a formal synthesis of psychotriasine.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Acetamides / chemistry*
  • Catalysis
  • Chloroacetates / chemistry*
  • Lewis Acids / chemistry*
  • Molecular Structure
  • Pyrroles / chemical synthesis*
  • Pyrroles / chemistry

Substances

  • Acetamides
  • Chloroacetates
  • Lewis Acids
  • Pyrroles
  • trichloroacetamide