Ruthenium-Catalyzed Synthesis of Quinazolinones through Hydrogen Transfer and Cyclization

An efficient ruthenium-catalyzed tandem cyclization for the formation of C-N bond was developed by using hydrogen transfer reaction and intramolecular cyclization. This process relied on the efficient availability of nitroarenes and primary alcohols to form C-N bond by hydrogen transfer reaction. This method could be widely used in the synthesis of quinazolinone skeletons due to less waste, higher reaction efficiency and better functional groups tolerance. A series of quinazolin-4(3H)-ones derivatives were obtained with high production by using nitroarenes and primary alcohols as the substrates. Finally, based on the experimental results, a reasonable series reaction mechanism was proposed.