Creating effective, ecologically friendly, and commercially viable synthetic routes is crucial in the design and synthesis of organic substances. Quinazoline, a heterocyclic compound with nitrogen, is one of the most significant heterocyclic motifs with diverse chemical reactivities and many biological applications. Its derivatives comprise a family of fused heterocycles in over 200 naturally occurring alkaloids. Over the past few decades, newer, more complex drugs containing quinazolinone structures have been discovered, with enormous progress in designing various efficient protocols to construct these pharmacologically active scaffolds. This review evaluated the recently investigated protocols for synthesizing quinazolines and their derivatives (from 2017 to 2023 till date). The current review paper provides an up-to-date description of recent advancements in straightforward synthetic procedures that result in the creation of quinazoline molecules. In addition, the significant therapeutical activities of numerous quinazoline-based drugs were briefed and assessed in this review. We envisage that this information would assist researchers in designing and synthesizing novel quinazoline analogues as lead compounds.

创造有效、生态友好且商业上可行的合成路线对于有机物质的设计和合成至关重要。喹唑啉是一种含氮杂环化合物，是最重要的杂环基序之一，具有多种化学反应性和许多生物学应用。其衍生物包含 200 多种天然生物碱中的稠合杂环家族。在过去的几十年里，含有喹唑啉酮结构的更新、更复杂的药物被发现，在设计各种有效的方案来构建这些药理活性支架方面取得了巨大进展。本综述评估了最近研究的喹唑啉及其衍生物的合成方案（2017 年至 2023 年至今）。当前的综述论文提供了对导致喹唑啉分子产生的简单合成程序的最新进展的最新描述。此外，本综述还介绍并评估了多种喹唑啉类药物的重要治疗活性。我们预计这些信息将有助于研究人员设计和合成新型喹唑啉类似物作为先导化合物。