Preparation of the Core Structure of Aspidosperma and Strychnos Alkaloids from Aryl Azides by a Cascade Radical Cyclization

Org Lett. 2016 Mar 18;18(6):1370-3. doi: 10.1021/acs.orglett.6b00306. Epub 2016 Feb 29.

Abstract

A novel approach to prepare the core structure of Aspidosperma and Strychnos alkaloids is described. The strategy is based on a cyclization cascade involving the formation of quaternary carbon center followed by trapping of the radical intermediate by an aryl azide to build the 5-membered ring of the pyrrolocarbazole system. This reaction is run with triethylborane without the need for any hydrogen atom donor such as a tin hydride or tris(trimethylsilyl)silane, and it furnishes the tetracyclic framework as a single diastereomer. The influence of different N-protecting groups on the starting iodoacetamide has been examined.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / chemical synthesis*
  • Alkaloids / chemistry
  • Aspidosperma / chemistry*
  • Azides / chemistry*
  • Catalysis
  • Cyclization
  • Indole Alkaloids / chemical synthesis
  • Indole Alkaloids / chemistry
  • Iodoacetamide / chemistry
  • Molecular Structure
  • Quinolines / chemical synthesis
  • Quinolines / chemistry
  • Stereoisomerism
  • Strychnine / chemical synthesis
  • Strychnine / chemistry
  • Strychnos / chemistry*

Substances

  • Alkaloids
  • Azides
  • Indole Alkaloids
  • Quinolines
  • aspidospermidine
  • Strychnine
  • Iodoacetamide