Diels-Alder Cycloaddition in Medicinal Chemistry

Diels-Alder reactions have emerged as highly powerful transformations for the generation of structurally complex polycyclic scaffolds essentially due to their associated rapidity and atom-economy. Since its discovery in 1928, a better understanding of steric and electronic effects have allowed the development of many different versions including intramolecular [4+2] cycloadditions, hetero-Diels-Alder reactions, and catalytic asymmetric variants, among others. In this chapter, we will give an overview on the application of Diels-Alder reactions in Medicinal Chemistry. Keywords: Diels-Alder reaction, [4+2] cycloaddition, medicinal chemistry, drug-like molecules, Diels-Alderase.