Abstract

A one-pot process involving cascade CH activation and insertion between amidines and alkynes in the presence of palladium salt is described. With this methodology, various novel eight-membered cyclopalladated amidines were efficiently constructed. Notably, a series of functionalities with potential application were readily accommodated under the reaction conditions. Isotope effects and H/D exchange suggested that this cascade is initiated by the cleavage of the ortho CH bond in the N-phenyl ring of amidines.

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