Total synthesis of exiguamines A and B inspired by catecholamine chemistry

Chemistry. 2012 Apr 16;18(16):4999-5005. doi: 10.1002/chem.201103605. Epub 2012 Mar 13.

Abstract

The evolution of a total synthesis of the exiguamines, two structurally unusual natural products that are highly active inhibitors of indolamine-2,3-dioxygenase (IDO), is described. The ultimately successful strategy involves advanced cross-coupling methodology and features a potentially biosynthetic tautomerization/electrocyclization cascade reaction that forms two heterocycles and installs a quaternary ammonium ion in a single synthetic operation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biological Products / chemical synthesis*
  • Biological Products / chemistry*
  • Catalysis
  • Catecholamines / chemistry*
  • Cyclization
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry*
  • Indole Alkaloids / chemical synthesis*
  • Indole Alkaloids / chemistry*
  • Indoleamine-Pyrrole 2,3,-Dioxygenase / antagonists & inhibitors*
  • Indoleamine-Pyrrole 2,3,-Dioxygenase / chemistry*
  • Indoles / chemical synthesis*
  • Indoles / chemistry*
  • Molecular Structure
  • Quinones / chemical synthesis*
  • Quinones / chemistry*
  • Spiro Compounds / chemical synthesis*
  • Spiro Compounds / chemistry*
  • Stereoisomerism

Substances

  • Biological Products
  • Catecholamines
  • Enzyme Inhibitors
  • Indole Alkaloids
  • Indoleamine-Pyrrole 2,3,-Dioxygenase
  • Indoles
  • Quinones
  • Spiro Compounds
  • exiguamine A
  • exiguamine B