Rapid access to difluoroalkyl phosphinimide heterocycles and their preliminary biological activities toward the cathepsin D active site

Abstract

An efficient Ir-catalyzed multicomponent photoredox radical addition/C–H activation/annulation reaction for the synthesis of “CF₂”-functionalized cyclic phosphinimides is reported. This strategy also enables the production of a library of phosphinimides with quaternary carbon centers by tolerating a range of radical species. Molecular docking simulations and experimental biological studies revealed that this type of CF₂-substituted phosphinimide binds to the cathepsin D active site. Some hits that were related to this target site were found from preliminary biological screenings.