Synthesis of hexahydropyrrolo[2,3-b]indole alkaloids based on the aza-Pauson-Khand-type reaction of alkynecarbodiimides

J Org Chem. 2007 Aug 31;72(18):6878-84. doi: 10.1021/jo071137b. Epub 2007 Aug 10.

Abstract

Upon treatment with 30 mol % of Co2(CO)(8) and 30 mol % of TMTU in toluene at 70 degrees C, benzene-bridged alkynecarbodiimides efficiently underwent a ring-closing reaction to give the pyrrolo[2,3-b]indol-2-ones in good yields. These conditions could nearly suppress the formation of the urea derivatives, which were consistently observed when 10 mol % of Co2(CO)(8) and 60 mol % of TMTU in benzene were used. The synthesis of the eight hexahydropyrrolo[2,3-b]indole alkaloids was accomplished from the resulting pyrrolo[2,3-b]indol-2-ones via the introduction of an angular substituent at the C(3a)-position by treatment with NaBH(4)/alkyl bromide as the crucial step.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Alkynes / chemistry*
  • Aza Compounds / chemistry*
  • Carbodiimides / chemistry*
  • Hydrogen / chemistry*
  • Indole Alkaloids / chemical synthesis
  • Indole Alkaloids / chemistry*
  • Molecular Structure
  • Pyrroles / chemistry*

Substances

  • Alkynes
  • Aza Compounds
  • Carbodiimides
  • Indole Alkaloids
  • Pyrroles
  • Hydrogen