The InnovationThis 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.
- 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
- 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 allows shortening synthetic pathways
Savings in economy and ecology
Minimizes use of solvents and can avoid some toxic reagents – regulatory issues solved