Synthesis of (±)-cis-clavicipitic acid by a Rh(I)-catalyzed intramolecular imine reaction

J Org Chem. 2014 Apr 4;79(7):3255-9. doi: 10.1021/jo500245s. Epub 2014 Mar 14.

Abstract

A new and short synthesis of racemic cis-clavicipitic acid was achieved by taking advantage of the double nucleophilic character of indole-4-pinacolboronic ester. Key to the success of the synthesis were an efficient and selective C-3 indole Friedel-Crafts alkylation and the development of an unprecedented intramolecular rhodium-catalyzed 1,2-addition of an aryl pinacolboronic ester to an unactivated imine.

MeSH terms

  • Alkylation
  • Boronic Acids / chemical synthesis*
  • Boronic Acids / chemistry*
  • Catalysis
  • Ergot Alkaloids / chemical synthesis*
  • Esters
  • Imines / chemistry*
  • Indoles / chemical synthesis*
  • Indoles / chemistry*
  • Molecular Structure
  • Rhodium / chemistry*
  • Stereoisomerism

Substances

  • Boronic Acids
  • Ergot Alkaloids
  • Esters
  • Imines
  • Indoles
  • clavicipitic acid
  • indole-4-pinacolboronic ester
  • indole
  • Rhodium