Artificial Macrocycles by Ugi Reaction and Passerini Ring Closure

J Org Chem. 2016 Oct 7;81(19):8789-8795. doi: 10.1021/acs.joc.6b01430. Epub 2016 Sep 15.

Abstract

Artificial macrocycles can be convergently synthesized by a sequence of an Ugi multicomponent reaction (MCR) followed by an intramolecular Passerini MCR used to close the macrocycle. Significantly, in this work, the first intramolecular macrocyclization through a Passerini reaction is described. We describe 21 macrocycles of a size of 15-20. The resulting macrocyclic depsipeptides are model compounds for natural products and could find applications in drug discovery.

Publication types

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

MeSH terms

  • Carbon-13 Magnetic Resonance Spectroscopy
  • Cyclization
  • Macrocyclic Compounds / chemistry*
  • Models, Chemical
  • Proton Magnetic Resonance Spectroscopy
  • Spectrometry, Mass, Electrospray Ionization

Substances

  • Macrocyclic Compounds