Abstract: Remote C-H bond functionalization of arenes with precise control is a recognized extraordinary challenge in organic synthesis. Recently, Yu and Houk et al. developed an elegant strategy to distinguish and functionalize remote C_sp²-H bonds of (hetero)arenes within one-bond distance by the interplay of a remote directing template and a transient norbornene-type mediator. A wide range of medicinally important benzoazines are well compatible with this method. The chemistry significantly expands the toolbox for site-selective functionalization of remote C_sp²-H bond of (hetero)arenes. This work has been published in Nature Chemistry in March, 2020.