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Copper-catalyzed C-H bond arylation in heterocycles and fluorobenzenes

The Innovation

The arylation of electron-rich and electron-poor heterocycles as well as polyflourinated aromatic compounds can be performed by using the combination of aryl halide, substrate, and a copper salt.

Competitive Edge

  • Previous methods based on C-H activation use rhodium or palladium catalysts.
  • Price differences between palladium or rhodium and copper: between 100- and 1000-fold
  • Generality: previous methods are successful only for a limited number of heterocycles; this method successful for a variety of substrates.
  • Use of C-H activation methodologies shortens synthetic pathways.
  • Savings in economy and ecology.
  • Minimizes use of solvents and can avoid some toxic reagents – regulatory issues solved.
  • Easier to separate copper than palladium from final product (drug purity issues solved).

Targeted Market

Chemical reagent manufacturers, oil and gas, emission control equipment manufacturers.