A direct access to heptasubstituted biguanides.

An efficient and experimentally simple copper-catalyzed carbon-nitrogen bond formation for the synthesis of [Formula: see text]-arylated biguanides starting from aryl halides, carbodiimides, and 1,1,3,3-tetramethylguanidine is reported. The potential diversity of this type of reaction, easily available starting materials, and commercially available low-cost catalysts are the incremental features of this methodology.