Using cheap, readily available, and economic active MnO2 as an oxidant, a series of 2,4-disubstituted quinazoline-3-oxides were synthesized in good to excellent yields by oxidation of the corresponding 1,2-dihydroquinazoline-3-oxides under mild conditions. This novel approach is simple and convenient and provides a series of 2,4-disubstituted quinazoline-3-oxides.