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Keywords:

  • 3-methyleneisoindolin-1-ones;
  • Cu(OAc)2·H2O;
  • 2,2′-biimidazole;
  • additive cyclization

Abstract

An efficient strategy for the synthesis of a variety of 3-methyleneisoindolin-1-ones has been developed. The reaction proceeded from coupling of 2-iodobenzamides (or 2-bromobenzamides) and terminal alkynes via Cu(OAc)2·H2O/2,2′-biimidazole catalyzed in DMF at 60°C and subsequent additive cyclization produced substituted 3-methyleneisoindolin-1-ones in good to excellent yields.