Quinazoline, as a common fused heterocyclic backbone, is an important structural unit in many pharmaceutical and agricultural molecules. Quinazoline derivatives possess a variety of biological activities, such as anticancer, anti-inflammatory, analgesic, anti-allergic, and antihypertensive activities. In addition, many quinazoline derivatives also exhibit excellent photophysical properties and can be used as fluorescent probes, bioimaging reagents, and luminescent materials.