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One of the most important challenges in medical society all over the world is cancer. The quinazoline-based compounds are versatile classes of fused heterocycles that are of considerable interest because of the diverse range of their biological applications such as anticancer, antibacterial and antifungal activity. The aim of this book is to develop new synthetic methods and design highly efficient, mild and selective organic reactions, as well as to investigate the mechanism to gain a deeper understanding of the corresponding reactions focused on strategies that enable reactions to proceed directly through C-S bond activation in the presence of cheap and easily available transition metal catalysts. It is certain that the remarkable advances in coupling chemistry that have been made in academic laboratories will be increasingly incorporated into industrial fine chemical and pharmaceutical preparations. In addition, the bioactivity researches of quinazoline derivatives were also discussed in order to provide a valuable reference for the future synthesis and biological investigation of these compounds.