Donor-Acceptor Cyclopropanes as 1,2-Dipoles in GaCl3-Mediated [4 + 2]-Annulation with Alkenes: Easy Access to the Tetralin Skeleton

J Org Chem. 2015 Aug 21;80(16):8225-35. doi: 10.1021/acs.joc.5b01179. Epub 2015 Jul 31.

Abstract

A new process for (4 + 2)-annulation of donor-acceptor cyclopropanes (DACs) with unsaturated compounds in the presence of anhydrous GaCl3 has been developed. In this process, DACs act as sources of formal 1,2- and 1,4-dipoles to give polysubstituted tetralins in high yields and with high regio- and diastereoselectivity. Alkenes with both aryl and alkyl substituents at the double bond undergo this reaction equally readily. A most likely mechanism of the reaction has been proposed. It involves preliminary generation of a key 1,2-dipolar gallium complex and its subsequent participation in annulation with an alkene.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkenes / chemistry*
  • Catalysis
  • Cycloaddition Reaction
  • Cyclopropanes / chemistry*
  • Gallium / chemistry*
  • Molecular Structure
  • Oxidation-Reduction
  • Stereoisomerism
  • Tetrahydronaphthalenes / chemistry*

Substances

  • Alkenes
  • Cyclopropanes
  • Tetrahydronaphthalenes
  • gallium chloride
  • Gallium