**Abstract**

4(3*H*)-Quinazolinone derivatives have considerable great interesting due to the diverse range of their biological properties. This review summarized the methods of preparation of 2-substituted-4(3*H*)-quinazolinone, 3-substituted-4(3*H*)-quinazolinone and 2,3-disubstituted-4(3*H*)-quinazolinone derivatives. Chemical reaction of 4(3*H*)-quinazolinone derivatives and the reactivity of the 2-methyl group, reactivity of the 3-amino group, electrophilic substitution, oxidation, reduction, reaction of 4(3*H*)-quinazolinones with metal ions, Mannich reaction, cycloaddition reaction as well as other reagents were discussed. Also, biological properties of 4(3*H*) quinazolinone derivatives were given herein.

**Keywords:** 4(3*H*)-quinazolinones, quinazolines, syntheses, reaction, biological activity
