BIPHEP and rac-BINAP are commonly employed in transition-metal-catalyzed bond formation. Their atropisomerically pure derivatives find traditional application in asymmetric hydrogenation and are increasingly utilized in asymmetric synthesis across various scaffold synthesis as ligands for metals such as Rhodium (Rh), Iridium (Ir), Palladium (Pd), Copper (Cu), and Gold (Au).

Their derivatives are meticulously designed by modulating the binding angel, steric hindrance and electronic properties to fine-tune their activity and adapt them for use with different substrates.