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Inspired by natural scaffolds, herein, we describe a practical and concise ligand\u2010enabled Pd(II)\u2010catalyzed sp\n                    <jats:sup>3<\/jats:sup>\n                    C\u2212H alkylation, olefination and arylation macrocyclization, which could offer a novel set of pseudo\u2010natural macrocyclic sulfonamides. Interestingly, the potential of ligand acceleration in C\u2212H activation is also demonstrated by an unprecedented enantioselective sp\n                    <jats:sup>3<\/jats:sup>\n                    C\u2212H alkylation macrocyclization. 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