A comprehensive review was conducted on the significance of 6-substituted quinazolin-4(3H)-ones and 2-substituted phenyl quinazolin-4(3H)-ones in medicinal and polymer chemistry, as well as the synthetic methodologies reported in the literature up to March 2016. The primary objective of our current investigation is to expand the chemical space of quinazolin-4(3H)-ones by introducing a series of biologically active molecules, specifically those featuring 6-aryl/heteroaryl or quinoxalinyl groups, as well as 6-functionalized acyclic substituents on the quinazolinone core. Additionally, we aim to design and synthesize hybrid molecules incorporating both quinazolinone and triazole scaffolds via dipolar cycloaddition reactions. Our synthetic strategy also extensively explores the application of Kumada coupling, Castro-Stephens coupling, and multicomponent reactions.