Controllable access to multi-substituted imidazoles via palladium(ii)-catalyzed C-C coupling and C-N condensation cascade reactions.

A novel and efficient protocol for the synthesis of various 2,4-disubstituted, 1,2,4-trisubstituted and 1,2,4,5-tetra-substituted imidazoles via cascade palladium catalyzed C-C coupling followed by intramolecular C-N bond formation was developed. Readily accessible boronic acids and N-substituted-2-aminoacetonitriles were firstly reported as starting materials to construct di-, tri-, and tetra-substituted imidazoles in good to excellent yield.