2-Aminopyrimidine

2-Anilinopyrimidine (2-AP) represents one of the most prevalent privileged scaffolds as a hinge-binding element. It is attracting the interest of medicinal chemists for the discovery of more kinase drugs. About 19 2-AP–derived kinase inhibitors were approved as therapeutic agents. In this chapter, we highlight advance and challenges of 2-AP–approved kinase drugs with an emphasis on discovery strategies and binding patterns.