Diversity-oriented synthesis (DOS) continues to grow as an important area in the disciplines of organic synthesis and chemical biology. One area that should benefit significantly from DOS is drug discovery. The existing chemical space can be expanded with new synthetic molecules, hoping to identify novel and better drug and probe molecules. Arguably, one of the most promising synthetic strategies for generating collections of small molecules by DOS involves the sequencing of multicomponent reactions (MCRs) with subsequent transformations, including cyclizations and refunctionalizations, that...