2-Methyl-3-o-tolyl-4 (3H)-quinazolinone (methaqualone, 3a), 2, 3-dimethyl-4 (3H)- quinazolinone (3b), and 2-methyl-3-phenyl-4 (3H))-quinazolinone (3c) were converted to the 2-lithiomethyl derivatives 4a, 4b, and 4c, respectively, by means of lithium diisopropylamide in THF-hexane at 0" C. Reactions of 4a-c with a series of electrophilic reagents led to elaboration at the original 2-methyl group. Thus, 4a was alkylated with methyl iodide, allyl ...