Aminocyclopropanes as precursors of endoperoxides with antimalarial activity

Org Biomol Chem. 2010 Dec 21;8(24):5591-601. doi: 10.1039/c0ob00308e. Epub 2010 Oct 11.

Abstract

This contribution describes the synthesis of several novel bicyclic α-amino endoperoxides, including CF(3)-substituted compounds, prepared by the aerobic electrochemical oxidation of a family of bicyclic aminocyclopropanes. These, in turn, are readily synthesised by a titanium-mediated intramolecular cyclopropanation process (Kulinkovich-de Meijere reaction), starting from N-alkenyl amides that contain a vic-disubstituted double bond, with high diastereoselectivity. An evaluation of the biological activities of several of the molecules produced, against the parasite Plasmodium falciparum, is also presented.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemistry
  • Amines / chemistry*
  • Antimalarials / chemical synthesis*
  • Crystallography, X-Ray
  • Cyclopropanes / chemical synthesis*
  • Cyclopropanes / pharmacology
  • Models, Molecular
  • Molecular Structure
  • Oxidation-Reduction
  • Peroxides / chemistry*
  • Plasmodium falciparum / drug effects
  • Structure-Activity Relationship

Substances

  • Amides
  • Amines
  • Antimalarials
  • Cyclopropanes
  • Peroxides
  • cyclopropane