An expedient route to a potent gastrin/CCK-B receptor antagonist (+)-AG-041R

J Org Chem. 2009 Oct 2;74(19):7522-4. doi: 10.1021/jo901352u.

Abstract

An enantiocontrolled synthesis of (+)-AG-041R (1), a potent gastrin/CCK-B receptor antagonist, has been achieved employing a chiral rhodium(II)-catalyzed, oxidative intramolecular aza-spiroannulation as the key step.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Indoles / pharmacology
  • Molecular Structure
  • Receptor, Cholecystokinin B / antagonists & inhibitors
  • Rhodium / chemistry
  • Stereoisomerism

Substances

  • AG-041R
  • Indoles
  • Receptor, Cholecystokinin B
  • Rhodium