Abstract
Three-component reaction of methyl α,α-disubstituted α-isocyanoacetates, primary amines, and aryl(vinyl) halides in the presence of Pd(OAc)2 (0.05 equiv) and Cu2O (1.0 equiv) provided 2,3,5,5-tetrasubstituted imidazolones via the formation of three chemical bonds. A copper-mediated migratory insertion of the isocyano group into the N-H bond of the amine followed by lactamization and Pd-catalyzed cross-coupling of the in situ generated amidinyl copper species with aryl(vinyl) halides accounted for the reaction outcome.
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