Directing group assists in transition metal‐catalyzed site‐selective C‐H bond activation/transformations

In the review paper, we attempt to point out the importance of the directing group in the transition metal‐catalyzed C‐H bond activation/transformations, especially in the site‐selectivity and reactivity. The employment of the directing groups in the type of reaction can enable a chemist to straightforwardly approach the desired molecular skeletons. Thus, understanding the role of the directing groups in the C‐H bond activation/transformations would benefit chemists to design better auxiliary groups and develop more efficient and practical synthetic methodologies. We believe that the synthetic strategy based on the utility of the directing group to assist in the transition metal‐catalyzed C‐H bond activation/transformations will keep playing as a mainstream role in the research field. The review paper mainly focuses on how the directing group assists the transition metals to catalyze the site‐selective C‐H bond activation and transformations. The contents include the introduction of the directing group, and the historical development of ortho‐, meta‐, and para‐C‐H bond activation/functionalizations.