Organocatalytic enantioselective formal synthesis of bromopyrrole alkaloids via aza-Michael addition

Org Biomol Chem. 2011 Oct 26;9(22):7734-41. doi: 10.1039/c1ob06078c. Epub 2011 Sep 27.

Abstract

An unprecedented organocatalytic enantioselective formal synthesis of bromopyrrole alkaloid natural products is reported. An organocatalytic aza-Michael addition using pyrroles as the N-centered nucleophile is utilized as the enantioselective step to construct the nitrogen-substituted stereogenic carbon center in bromopyrrole alkaloids in good yield and excellent enantioselectivity. The aza-Michael product is converted via lactamization using a Staudinger-type reductive cyclization to the key intermediate, which was previously used in the total synthesis of bromopyrrole alkaloid natural products.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / analysis
  • Alkaloids / chemical synthesis*
  • Animals
  • Anti-Bacterial Agents / analysis
  • Anti-Bacterial Agents / chemical synthesis*
  • Aquatic Organisms / chemistry
  • Bromides / chemistry
  • Catalysis
  • Chemistry, Pharmaceutical / methods*
  • Cyclization
  • Lactams, Macrocyclic / chemistry
  • Molecular Structure
  • Porifera / chemistry
  • Pyrroles / chemistry*
  • Stereoisomerism

Substances

  • Alkaloids
  • Anti-Bacterial Agents
  • Bromides
  • Lactams, Macrocyclic
  • Pyrroles