Syntheses of beta,beta-difluorotryptamines

J Org Chem. 2003 Apr 4;68(7):2798-802. doi: 10.1021/jo020731c.

Abstract

Tryptamines disubstituted at the beta-position with fluorine have been synthesized as part of our research program to study the effects of fluorine substitution on the biological activities of neuroactive amines. Treatment of N-Boc-3-azidoacetyl indoles, prepared from readily available 2-chloracetylindoles, with dimethoxyethylamino sulfurtrifluoride produced the corresponding 3-(2-azido-1,1-difluoroethyl)indoles. Reduction of the azide to amine with hydrogen over Pd-C and careful removal of the N-Boc protecting group produced beta,beta-difluorotryptamines.

MeSH terms

  • Catalysis
  • Combinatorial Chemistry Techniques
  • Formic Acid Esters / chemistry
  • Hydrocarbons, Fluorinated / chemical synthesis*
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Oxidation-Reduction
  • Stereoisomerism
  • Structure-Activity Relationship
  • Tryptamines / chemical synthesis*

Substances

  • Formic Acid Esters
  • Hydrocarbons, Fluorinated
  • Tryptamines
  • t-butyloxycarbonyl group