Enantioselective synthesis of dihydro-1H-benzindoles

J Org Chem. 2013 Apr 5;78(7):3379-83. doi: 10.1021/jo302798j. Epub 2013 Mar 22.

Abstract

The first examples of dihydro-1H-benzindoles by enantioselective γ-lactamization reaction of naphthyl sulfilimines with trichloroacetyl chloride in the presence of ZnCu as catalyst (≥98:2 er and 65-80% yields) are described. Products are obtained by [3,3]-sigmatropic rearrangement of the azasulfonium enolate or followed by a second allylic rearrangement that transfers chirality. The absolute stereochemistry was confirmed by X-ray crystallography, which provides support for the mechanisms proposed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Chloroacetates / chemistry*
  • Copper / chemistry
  • Crystallography, X-Ray
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Models, Molecular
  • Molecular Structure
  • Stereoisomerism
  • Zinc / chemistry

Substances

  • Chloroacetates
  • Indoles
  • Copper
  • trichloroacetyl chloride
  • Zinc