Ring-opening cyclization of cyclohexane-1,3-dione-2-spirocyclopropanes with amines: rapid access to 2-substituted 4-hydroxyindole

Org Lett. 2014 Aug 1;16(15):4012-5. doi: 10.1021/ol501837b. Epub 2014 Jul 17.

Abstract

An efficient ring-opening cyclization of cyclohexane-1,3-dione-2-spirocyclopropanes with primary amines has been developed. The reaction proceeded at room temperature without any additives to provide 2-substituted tetrahydroindol-4-ones in good to excellent yields without the formation of the 3-substituted isomers. The obtained product was readily converted into a 2-substituted 4-hydroxyindole derivative via a synthetically useful indoline intermediate.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amines / chemistry*
  • Catalysis
  • Combinatorial Chemistry Techniques
  • Cyclization
  • Cyclohexanes / chemistry*
  • Cyclopropanes / chemistry*
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Molecular Structure
  • Spiro Compounds / chemistry*
  • Stereoisomerism

Substances

  • Amines
  • Cyclohexanes
  • Cyclopropanes
  • Indoles
  • Spiro Compounds
  • 4-hydroxyindole
  • Cyclohexane