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MCRs are very useful reactions for the rapid generation of complex and diverse molecules in a very efficient way. In this book, the use of these reactions as a platform for the generation of structural or skeletal diversity is studied in more details. In addition, the potential of the 3CR toward some heterocyclic compounds predicting to have a biological activities is described. Chromenes, pyranopyrridines, pyrano[3,2-b]pyrrole derivatives and some other heterocyclic compounds have been synthesized via catalyzed MCRs.