2-a]benzimidazoles, which show interesting and potentially useful biological activities, have drawn extensive attention from chemists. A straightforward copper acetate-oxidative one-pot synthesis of these compounds from 2-aminopyridines and phenylboronic acids through C–Nbondformation and C–Hbondactivation was developed as a simple and convenient method.
A simple and efficient method for the preparation ofpyrido[1,2-a]benzimidazoles by a copper-catalyzed inter- and intramolecular C–Ncouplingcascadeprocess was designed and carried out, and the products were obtained in moderate to excellent yields (up to 93 %).