Regioselective dibromination of methyl indole-3-carboxylate and application in the synthesis of 5,6-dibromoindoles

Org Biomol Chem. 2011 Jul 21;9(14):5021-3. doi: 10.1039/c1ob05522d. Epub 2011 Jun 3.

Abstract

Treatment of methyl indole-3-carboxylate with bromine in acetic acid gives methyl 5,6-dibromoindole-3-carboxylate regioselectively, from which the parent 5,6-dibromoindole can be accessed via a one-pot, microwave-mediated ester hydrolysis and decarboxylation. Application of these building blocks in syntheses of natural and non-natural 5,6-dibromoindole derivatives, including meridianin F and 5,6-dibromo-2'-demethylaplysinopsin, is reported.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetic Acid / chemistry
  • Bromine / chemistry*
  • Indoles / chemical synthesis*
  • Indoles / chemistry*
  • Molecular Structure
  • Stereoisomerism

Substances

  • Indoles
  • Acetic Acid
  • Bromine