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Use of aryl chlorides in palladium-catalyzed C-H bond functionalization

The Innovation

This method will allow the shortening of synthetic schemes leading to several top-selling drugs. The method allows the direct arylation of C-H bonds by cheap chloroarenes by using palladium catalysts.

Competitive Edge

  1. Previous methods based on C-H activation use rhodium catalysts and/or aryl bromide/iodide reagents
    Price differences between aryl iodides and aryl chlorides: more than order of magnitude; between rhodium and palladium catalysts: ca. 5 times
  2. Generality: previous methods are successful only for a limited number of heterocycles; this method successful for a variety of substrates
  3. Use of C-H activation methodologies allows shortening synthetic pathways
    Savings in economy and ecology
    Minimizes use of solvents and can avoid some toxic reagents – regulatory issues solved

Targeted Market

Drug companies.