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4(3H)-Quinazolinone derivatives have considerable interest due to the diverse range of their biological properties. This method of preparation of 2-methyl-4(3H)-quinazolinone, 3-substituted-4(3H)-quinazolinone and 2,3-disubstituted-4(3H)-quinazolinone derivatives. The chemical reaction between anthranilic acid and acetyl chloride followed by dehydration to form the benzoxazinone intermediate; subsequent addition of a p-amino acetophenone provided the fused 3-(4-acetylphenyl)-2-methylquinazolin-4-one. The various chalcones ( 2a – j ) were prepared by condensation of compound ( 1 ) with the appropriate aromatic aldehydes. Compounds ( 2a – 2j ) react with hydrazine hydrate to form ( 3a–3j ), hydrazine hydrates along with formic acid to form compounds ( 4a–4j) which are substituted 4(3H)quinazolinones as depicted in Scheme 1. The structures of the newly synthesized compounds were confirmed by IR, 1 H-NMR and Mass spectroscopy and Elemental analyses. Acute toxicity study of synthesized compound was found according to OECD guidelines 423. The test compound does not show any toxicity up to 50mg/kg dose.