Fused quinazolinone derivatives can be found both in naturally occurring alkaloids and in a number of pharmaceutically active substances. Among them pyrrolo[1,2-a]quinazolines, the structural izomers of Peganine system, had attracted especial attention of the chemists. Structures containing the latter heterocyclic core with analgesic, antihypertensive and CNS depressing activities were discovered. The classical approach to the pyrrolo[1,2-a]quinazoline ring synthesis is to alkylate 2-aminobenzoic acid esters or nitriles with 4-halobutanenitrile derivatives. A few less common methods were reported, for example reactions of aminobenzoic acid (anthranilic acid) amides with 2-oxoglutaric acid and 4-oxopentanoic (levulinic) acid. It was found that anthranilic acid N-acylhydrazides, prepared from the reaction of isatoic anhydride with benzoic, 3-bromobenzoic, 2-hydroxy benzoic (salicylic), isonicotinic and nocotinic acid hydrazides, were useful instead of amides. The reactions of 2-oxoglutaric acid and 4-oxopentanoic (levulinic) acid with hydrazides of anthranilic acid in the refluxing acetic acid were found to give 3a-substituted 4-acylaminopyrrolo[1,2-a]quinazolines in good yields (71-85%). Performing the reactions using hydrazides, the synthesized pyrroloquinazoline derivatives contain CO-N-N fragment that is characteristic of pharmaceutically active substances. Furthermore, the utilization of oxoacids allows the incorporation of COOH and CH3 groups, permitting possibility of their additional functionalization, and applicatibility for further chemical transformations.