Host-Guest Interaction-Controlled Site-selective C–H Borylation of Aromatic Compounds

The site-selective transformation of aromatic compounds remains a challenge in organic synthesis. Conventional methods for controlling site-selectivity often use directing groups, which limit substrate availability owing to the need for coordinating functional groups. Herein, we report a strategy in which the cyclic moiety of a catalyst recognizes and traps the substrate via host-guest interaction between the catalyst and substrate, allowing the catalytically active site to preferentially approach the desired reaction site, thereby enabling site-selective reactions. This catalyst can be used to control the site-selectivity of substrates that lack functional groups, which are essential in conventional methods. These results have the potential to extend the substrate scope and provide new catalyst designs for carbon–hydrogen bond transformations.