A series of 2-substituted-2,3-dihydro-4(1H)-quinazolinones derivatives were synthesized efficiently by the cyclocondensation of 2-anthranilamide with an aldehyde or ketone in the presence of aluminum chloride in water at 60 ℃ after grinding at room temperature. The catalytic activity of different catalysts was compared. The effects of the amount of catalyst and the amount of solvent on the yields were investigated. The results show that the best reaction results could be obtained when the molar ratio of 2-anthranilamide to an aldehyde or ketone is 1∶1, the amount of catalyst is 1% (based on the mole of reactant), and water is 2 mL. The structures of products were characterized by IR, 1H-NMR, mass spectrum and elemental analysis. The probable catalytic mechanism for the reaction was proposed.