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Keywords:

  • arylation;
  • C[BOND]C coupling;
  • fused-ring systems;
  • microwave chemistry;
  • palladium;
  • regioselectivity
Thumbnail image of graphical abstract

Highly regioselective: An efficient synthesis of the imidazo[1,2-b]pyrazole core has been developed, and the first regioselective palladium-catalyzed direct arylation of the C-3 position is described (see scheme). Good to excellent yields were obtained for a wide range of aryl partners with electron-rich and electron-poor substituents. This methodology allows rapid access to a large variety of imidazo[1,2-b]pyrazole products and could open the way to the design of new biologically active compounds.