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Multiple bond-forming transformations (MBFTs) involving multicomponent reactions (MCRs) can be defined as processes in which three or more reactants introduced simultaneously are combined through covalent bonds to form a single product, regardless of mechanisms and protocols involved. Since MCRs are often highly compatible with a range of unprotected orthogonal functional groups, on a second level, scaffold diversity of MCR can be greatly enhanced by introduction of orthogonal functional groups into primary MCR product and react them in subsequent transformations, for example, ring-forming reactions. Some classes of densely functionalized small molecules have been shown to be particularly suited for use in these transformations, and in this context 1,2- and 1,3-dicarbonyl compounds are exceptional synthetic platforms. The rapid and easy access to biologically relevant compounds by MCRs and their scaffold diversity have been recognized by synthetic community in industry and academia as a preferred method to design and discover biologically active compounds.

Original publication





Book title

Stereoselective Multiple Bond-Forming Transformations in Organic Synthesis

Publication Date



423 - 446