Abstract A series of novel thioglycoside derivatives containing 4 (3H)-quinazolinone was designed and synthesized from 2-chloromethyl-quinazolin-4 (3H)-ones and 1-thioglycose. Several 2-chloromethyl-quinazolin-4 (3H)-ones were synthesized on refluxing with 2- (chloroacetylamino)-benzoic acid and arylamines in acetonitrile. All of the novel compounds were characterized by IR, 1 H NMR spectra and elemental analysis. The structures of ...