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Multi-component reactions are very popular because they offer a wealth of products, while requiring only a minimum effort combining many elements of an ideal synthesis, such as operational simplicity, atom economy, bond-forming efficiency, and the access to molecular complexity from simple starting materials. As such, multi-component reactions have become the cornerstones of both combinatorial chemistry and diversity-oriented synthesis and thus playing a central role in the development of modern synthetic methodology for pharmaceutical and drug discovery research. In this Insight we will highlight the development of novel multi-component reactions based on the reactivity of carbodiimides, paying particular attention on their mechanistic features. We will address our attention on the process developed by us and others groups, in these last years, for the synthesis of biologically relevant structures such as, for example, heterocycles and glyco-conjugates.
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