Even though several quinazolinone derivatives have been synthesized, still there is a constant demand for designing and synthesis of new quinazolinone derivatives by fine‐tuning the electronic and steric properties of substituents due to their interesting structure‐based biological utilities and the versatile chemistry. While many of the synthetic routes are useful as building blocks in synthetic organic chemistry, the drawbacks of some of these methods like unsatisfactory or variable yields, prolonged reaction times, inadequate tolerance to other substrates, including the use of costly catalysts/reagents. This review article is mainly focused on various synthetic routes for the preparation of quinazolinones, their important properties and applications.