Multicomponent Reactions in Medicinal Chemistry

Multicomponent reactions (MCRs) provide an alternative scheme for target synthesis, by allowing fast and efficient synthetic target access based on its “one-pot” character, accessing an almost unlimited scaffold diversity, by fostering a very large chemical space based on simple building blocks available in numerous derivatives, and by addressing challenging issues of sustainability (“green chemistry”). Hence, MCR can be potentially very useful in the discovery and synthesis of biologically active “drug-like” compounds. Here, we highlight examples of the use of MCR in medicinal chemistry, from drug discovery, synthesis of drugs, to screening libraries and biopharmaceutical applications. The review is not comprehensive but is rather based on a personal selection of the authors to provide the reader an overview on the advantages and usefulness of MCR. We conclude that the literature analysis, in toto, supports a highly underused role for MCR in medicinal chemistry.