Ruthenium-Catalyzed Aminocarbonylation with Isocyanates Through Weak Coordinating Groups

Introducing amide functional groups under mild conditions has growing importance owing to the prevalence of such moiety in biologically active molecules. Herein, we disclose a mild protocol for the directed ruthenium-catalyzed C-H aminocarbonylation with isocyanates as the amidating agents developed through high-throughput experimentation (HTE). The redox-neutral and base-free reaction is guided by weakly Lewis basic functional groups, including anilides, lactams and carbamates to access anthranilamide derivatives. The synthetic utility of this transformation is reflected by large-scale synthesis and late-stage functionalization. Under mild conditions: A redox-neutral and base-free protocol for the directed ruthenium-catalyzed C-H aminocarbonylation is developed through high-throughput experimentation. The mild conditions allowed the introduction of privileged amide moieties to a wide range of anilides bearing various substitution patterns and different weakly Lewis basic directing groups.image