Abstract: Reaction of 2-(chloromethyl)-3-arylquinazolin-4 (3H)-one 3 with N-BOC piperazine 4 in acetonitrile using K 2 CO 3 and KI, followed by deprotection of BOC group in IPA HCl, gives 3-aryl-2-(piperazin-1-yl) quinazolin-4 (3H)-one 6. The latter on treatment with benzene/methane sulfonyl chloride in DCM in the presence of TEA at RT, results in the formation of 2-(4-benzene/methane sulfonylpiperazin-1-yl-methyl)-3-aryl-quinazolin-4 (3H ...