Development of nonproprietary catalysts for the palladium-catalyzed amination reaction

ORGN 281

Robert A. Singer, robert.a.singer@pfizer.com, Chemical Research and Development, Pfizer Inc, Eastern Point Road, Bldg. 118C, room C415B, Groton, CT 06340
Recently, we have been involved in developing easily prepared phosphine ligands which can be applied to the Pd-catalyzed amination reaction. We initiated our own program at Pfizer to ensure our freedom to operate in this area and to identify ligands that could be readily prepared in bulk quantity. Our most efficient phosphines are derived from aryl pyrazoles and rely on a directed lithiation to install a di-t-butylphosphine moiety. We will report on our most current efforts in this area including optimization of use of our commercially available BippyPhos ligand.