Ahmed A. Noser, Esraa Saeed Abbas, Mohanad Mousa Kareem, Maha M. Salem
Abstract Heterocyclic compounds are very important in medicinal chemistry. One of the most significant heterocycles in this field is quinazolinones, which exhibit a wide range of medical applications such as anticancer, antimicrobial, anti‐inflammatory, antiviral, and antidiabetic effects. This review emphasizes recent advances in the new synthesis of quinazolinone derivatives using both conventional and green methods and demonstrates some of the chemical reactions related to quinazolinones. Additionally, we explore some medical and industrial applications of quinazolinones. This evaluation identifies the period from 2013 to 2025 as a pivotal era for quinazolinone research, connecting traditional synthetic techniques with modern sustainable approaches. We present an innovative strategy that links chemical techniques to therapeutic efficacy by evaluating the shift from high‐waste traditional methods to energy‐efficient green protocols.