Spirobipyridine Ligand Enabled Iridium‐Catalyzed Site‐Selective C‐H Activation via Non‐Covalent Interactions

The selective borylation of specific C‐H bonds in organic synthesis remains a formidable challenge. In this study, we present a novel spirobipyridine ligand that features a binaphthyl backbone. This ligand facilitates the iridium‐catalyzed selective C‐H borylation of benzene derivatives. The ligand is designed with "side‐arm‐wall" substituents that allow vicinal di‐ or multi‐substituted benzene derivatives to approach metal center and effectively block other reactive sites by non‐covalent interactions with substrates. The effectiveness of this strategy is demonstrated by the successful selective distal C‐H activation of various alkaloids and its broad compatibility with functional groups.