A one-pot process for synthesis of eight-membered cyclopalladated amidines via cascade C-H activation and insertion

A one-pot process involving cascade C-H 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 C-H bond in the N-phenyl ring of amidines. (C) 2020 Elsevier B.V. All rights reserved.