posted on 2010-11-05, 00:00authored byCarlos Mateos, Javier Mendiola, Mercedes Carpintero, José Miguel Mínguez
A highly regioselective Pd-catalyzed arylation of N-methylpyrazoles with aryl bromides is described. This transformation was studied extensively via automated reaction screening. A Design of Experiments (DoE) approach for optimizing the critical parameters was applied, resulting in excellent conditions for preparing selectively 5-arylpyrazoles in moderate to excellent yields under mild conditions.