Ruthenium‐Catalyzed N‐Alkylation for the Synthesis of 2‐ N ‐Pyridylmethyl Benzonitriles and an Exploration of Its Synthetic Utility

The N‐alkylation of 2‐aminobenzonitriles with pyridyl methanols as the alkylating reagents has been demonstrated by using an easily available Ru 3 (CO) 12 /Binap/ t BuOK [Binap=2,2′‐bis(diphenylphosphino)‐1,1′‐binaphthyl] catalyst system. The synthetic protocol can be used to synthesize various 2‐ N ‐pyridylmethyl benzonitriles in moderate to good isolated yields. Through an exploration of its synthetic utility, we have demonstrated a novel straightforward synthesis of biologically interesting 2,3‐diaryl‐1,2,3,4‐tetrahydrobenzo[ e ][1,4]diazepin‐5‐ones, which provides an important basis for the discovery of new bioactive compounds.