(A) Desymmetrization of prochiral C(sp3)–H bonds on the two different carbon centers. (B) Two synthetic disconnections. (C) Differentiating methylene C(sp3)–H bond on the same carbon center. DG, directing group; PG, protecting group; OTf, trifluoromethanesulfonate; Ar, aryl group; Ac, acetyl group; Et, ethyl group; Bu, butyl group.