Conformation-driven C3-C( sp 3 )–H arylation of saturated azacycles using Pd catalyst (opens in new tab)

Directed Pd-catalysed site-selective C(sp3)–H activation offers an effective route to functionalized amines that are highly valued yet synthetically challenging in drug discovery. Despite the central importance of diverse saturated azacycles in biologically active molecules, a general strategy harnessing native endocyclic nitrogen that only works for specific types of conformation as the directing element for C–H activation of these scaffolds has remained unsolved due to conformational constr...