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The development of environment‐friendly, step economic couplings to generate structurally diverse macrocyclic compounds is highly desirable but poses a marked challenge. Inspired by the C−H oxidation mechanism of cytochromes P450, an unprecedented and practical RhIII‐catalyzed acylmethylation macrocyclization via C−H/O2 dual activation has been developed by us. The process of macrocyclization is facilitated...
The development of environment‐friendly, step economic couplings to generate structurally diverse macrocyclic compounds is highly desirable but poses a marked challenge. Inspired by the C−H oxidation mechanism of cytochromes P450, an unprecedented and practical RhIII‐catalyzed acylmethylation macrocyclization via C−H/O2 dual activation has been developed by us. The process of macrocyclization is facilitated...