Development of nonproprietary phosphine ligands for the Pd-catalyzed amination reaction

A new family of pyrazole and bi-pyrazole phosphine ligands are reported that perform efficiently in the Pd-catalyzed amination reaction. Of the ligands screened, ligand 1 emerged as the most compatible for couplings involving both primary and secondary amines with typical yields of 84-99%.

We have prepared a new family of pyrazole and bi-pyrazole phosphine ligands that perform efficiently in the Pd-catalyzed amination reaction. Of the ligands screened, ligand 1 is the most compatible for couplings involving both primary and secondary amines with typical yields of 84-99%.