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Keywords:

  • acetylenes;
  • copper;
  • cyclization;
  • indoles
Thumbnail image of graphical abstract

Air and water welcomeligands need not apply! A simple and efficient new synthesis of variously functionalized and substituted indoles was achieved by the addition and copper-catalyzed coupling of N-formyl-o-haloanilines with acetylenic sulfones, esters and ketones (see scheme; EWG=electron-withdrawing group). The reaction employs copper(II) acetate under ligand-free conditions without the need for exclusion of air and moisture.