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Synthesis of 4-(trifluoromethyl)thiocoumarins

  • A. S. Golubev,
  • I. M. Golubev,
  • P. N. Ostapchuk,
  • T. V. Strelkova,
  • K. Yu. Suponitsky,
  • N. D. Chkanikov

摘要

A convenient method for the synthesis of poorly studied 4-(trifluoromethyl)thiocoumarins from 1-[2-(tert-butylthio)phenyl]-2,2,2-trifluoroethanones was developed. Thiopyranone core of 4-(trifluoromethyl)thiocoumarins was constructed by S-acylation of 1-[2-(tert-butylthio)phenyl]-2,2,2-trifluoroethanones with bromoacetyl bromide followed by treatment with triphenylphosphine to give the phosphonium salt and subsequent intramolecular Wittig reaction. S-Acylation of these substrates with acetyl chlorides bearing active methylene group and subsequent intramolecular Knövenagel condensation gave 3-substituted 4-(trifluoromethyl)thiocoumarins.