o‐Alkenylation of unprotected phenols has been developed by direct C−H functionalization catalyzed by PdII. This work features phenol group as a directing group and realizes highly site‐selective C−H bond functionalization of phenols to achieve the corresponding products in moderate to excellent yields at 60 °C. The advantages of this reaction include unprecedented C−H functionalization using phenol as a directing group, high regioselectivity, good substrate scope, mild reaction conditions, and high efficiency. To the best of our knowledge, this is the first example of a regioselective C−H alkenylation of unprotected phenols utilizing phenolic hydroxyl group as a directing group. The alkenylation of unprotected tyrosine and intramolecular cyclization are also successfully carried out under this catalytic system in good yields. Furthermore, this novel method enables a late‐stage modification of complex phenol‐containing bioactive molecules toward a diversity‐oriented drug discovery.

A simple and efficient copper(II)‐catalyzed C5 azidation of N‐acylated 8‐aminoquinolines by remote C−H activation was developed. On the basis of this reaction, a series of new C5‐azidated 8‐amidequinolines were synthesized in moderate to good yields.

We report herein the first example of Cu(II)-catalyzed site selective azidation of aromatic amines via C-H functionalization in aqueous media. In our strategy, a mild reagent was utilized. HO served as the oxidant, and sodium azide was used as the azidation reagent. This method could also be applied to late-stage functionalization of drugs that possess an aromatic amine moiety. In addition, we found that bromination or iodination on the ortho-position of aromatic amines could occur efficiently using this catalytic system.

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A novel chemiluminescent probe based on intramolecular cyclization for hydrazine detection in living cells.