Rh(III)-Catalyzed Double C–H Activation toward\nPeptide–Benzazepine Conjugates

We\nherein report the efficient synthesis of peptide–benzazepine\nconjugates from Lys-based peptides and acroleins via Rh(III)-catalyzed\ndouble C–H activation. This reaction features mild reaction\nconditions, broad scope, high atom and step economies, and excellent\nchemo- and site selectivity. The synthetic utility of this strategy\nis further demonstrated by scale-up experiments and product derivatizations,\nincluding diverse late-stage ligations based on the aldehyde moiety.\nThe preliminary biological activity studies show that peptide–benzazepine\nconjugates have good antifungal activities toward crop and forest\npathogenic fungi.