Transition metal–catalyzed aryl C−H activation is a powerful synthetic tool as it offers step and atom-economical routes to site-selective functionalization. Compared with proximal ortho-C−H activation, distal (meta- and/or para-) C−H activation remains more challenging due to the inaccessibility of these sites in the formation of energetically favorable organometallic pretransition states. Directing the catalyst toward the distal C−H bonds requires judicious template engineering and catalyst design, as well as prudent choice of ligands. This review aims to summarize the recent elegant discoveries exploiting directing group assistance, transient mediators or traceless directors, noncovalent interactions, and catalyst and/or ligand selection to control distal C−H activation.

过渡金属催化的芳基CH活化是一种功能强大的合成工具，因为它提供了位点选择性官能化的分步和原子经济途径。与近端邻位CH激活相比，远端（间位和/或对位）-）CH活化仍然更具挑战性，因为这些位点在形成能量上有利的有机金属预过渡态时难以接近。将催化剂引向末端CH键需要明智的模板设计和催化剂设计，以及谨慎的配体选择。这篇综述旨在总结最近的发现，这些发现是利用引导基团的协助，瞬时介体或无痕导向子，非共价相互作用以及催化剂和/或配体的选择来控制远端CH活化的。