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Contents: L. Banfi ∙ A. Basso ∙ R. Riva: Synthesis of Heterocycles Through Classical Ugi and Passerini Reactions Followed by Secondary Transformations Involving One or Two Additional Functional Groups.- V.A. Chebanov ∙ K. A. Gura ∙ S.M. Desenko: Aminoazoles as Key Reagents in Multicomponent Heterocyclizations.- Y. Huang ∙ K. Khoury ∙ A. Dömling: Piperazine Scaffolds by Multicomponent 3 Reactions: The Piperazine Space 4 in MCR Chemistry 5 Deep MCR Piperazine Space.- N. Elders ∙ E. Ruijter ∙ V.G. Nenajdenko ∙ R.V.A. Orru: α-Acidic Isocyanides in Multicomponent Chemistry.- A. Cukalovic ∙ J.-C.M.R. Monbaliu ∙ C.V. Stevens: Microreactor Technology as an Efficient Tool for Multicomponent Reactions.- L.A. Wessjohann ∙ C.R.B. Rhoden ∙ D.G. Rivera ∙ O. Eichler Vercillo: Cyclic Peptidomimetics and Pseudopeptides from Multicomponent Reactions.- M. del Mar Sanchez Duque ∙ C. Allais ∙ N. Isambert ∙ T. Constantieux ∙ J. Rodriguez: ß-Diketo Building Blocks for MCRs-Based Syntheses of Heterocycles

Comprehensive and up-to-date, this book focuses on the latest advances in the field, such as newly developed techniques, more environmentally benign processes, broadened scopes, and completely novel MCRs. In addition to carbene-promoted MCRs and frequently applied metal-catalyzed MCRs, it also covers recently developed catalytic enantioselective variants as well as MCR in drug discovery and for the synthesis of heterocyclic molecules and macrocycles. Edited by the leading experts and with a list of authors reading like a "who's who" in multicomponent reaction chemistry, this is definitely a must-have for every synthetic organic chemist as well as medicinal chemists working in academia and pharmaceutical companies.

The efficacy of isocyanide reactions in the synthesis of natural or naturallike products has resulted in a renaissance of isocyanide chemistry. Now isocyanides are widely used in different branches of organic, inorganic, coordination, combinatorial and medicinal chemistry. This invaluable reference is the only book to cover the topic in such depth, presenting all aspects of synthetic isonitrile chemistry. The highly experienced and internationally renowned editor has brought together an equally distinguished team of authors who cover multicomponent reactions, isonitriles in total synthesis, isonitriles in polymer chemistry and much more.

Géraldine Masson, Luc Neuville ∙ Carine Bughin ∙ Aude Fayol ∙ Jieping Zhu Multicomponent Syntheses of Macrocycles Thomas J.J. Müller Palladium-Copper Catalyzed Alkyne Activation as an Entry to Multicomponent Syntheses of Heterocycles Rachel Scheffelaar ∙ Eelco Ruijter ∙ Romano V.A. Orru Multicomponent Reaction Design Strategies: Towards Scaffold and Stereochemical Diversity Nicola Kielland ∙ Rodolfo Lavilla Recent Developments in Reissert-Type Multicomponent Reactions Jitender B. Bariwal ∙ Jalpa C. Trivedi ∙ Erik V. Van der Eycken Microwave Irradiation and Multicomponent Reactions Irini Akritopoulou-Zanze ∙ Stevan W. Djuric Applications of MCR-Derived Heterocycles in Drug Discovery

This timely book provides a succinct summary of methods for the synthesis of bioactive heterocycles using a multicomponent reaction (MCR) approach. The majority of pharmaceuticals and biologically active agrochemicals are heterocycles while countless additives and modifiers used in industrial applications are heterocyclic in nature. With the recent introduction of high-throughput biological evaluation, the importance of MCRs for drug discovery has been recognized and considerable efforts have been focused especially on the design and development of multi-component procedures for the generation of various bioactive heterocycles due to their significant therapeutic potential.

Presents a wide-ranging overview of essential topics and recent advances in MCR chemistry Heterocycles are a central component in natural product chemistry, pharmaceuticals, agrochemicals, and material science. New synthetic methodologies integrating the sequencing of multicomponent reactions (MCRs) are today being used for the rapid synthesis of diversified heterocycles in just one step. Multicomponent Reactions towards Heterocycles presents an up-to-date summary MCR chemistry with a focus on the conjugation between modern synthetic methodologies and MCRs. Featuring contributions by leaders in the field, this comprehensive resource highlights applications of MCRs in natural products and intermediate synthesis, discusses current trends and future prospects in MCR chemistry, outlines novel multicomponent procedures, and more. The authors provide the practical information required for designing new reaction strategies and mechanisms, covering topics including MCR-based green synthetic methods, cyclization and cycloaddition reactions, heterocycle multicomponent syntheses in a continuous flow, catalytic alkynoyl generation, MCR synthesis of saturated heterocycles, and C–H functionalization and multicomponent reactions. Provides a thorough overview of heterocycles as input in multicomponent reactions Discusses recent advances in the field of MCR chemistry and progress in the synthesis and functionalization of heterocycles Demonstrates the use of MCRs to simplify synthetic design and achieve complexity and diversity in novel bioactive molecules Highlights examples of multicomponent polymerizations, target-oriented synthesis, and applications of MCR in medicinal chemistry Explains the methodology of using on-resin MCRs to produce heterocycle compounds Illustrating the key role of MCRs towards heterocycles in natural product synthesis, drug discovery, organic synthesis, and other applications, Multicomponent Reactions towards Heterocycles is required reading for synthetic chemists in academia and industry alike.

Addressing a dynamic aspect of organic chemistry, this book describes synthetic strategies and applications for multicomponent reactions – including key routes for synthesizing complex molecules. • Illustrates the crucial role and the important utility of multicomponent reactions (MCRs) to organic syntheses • Compiles novel and efficient synthetic multicomponent procedures to give readers a complete picture of this class of organic reactions • Helps readers to design efficient and practical transformations using multicomponent reaction strategies • Describes reaction background, applications to synthesize complex molecules and drugs, and reaction mechanisms

Isocyanide based multicomponent reactions, including the Ugi four-component and Passerini three-component reactions, offer chemists a powerful tool for quickly constructing complex molecules. A particular form of the Ugi reaction, in which two of the four reacting components are introduced into a single molecule, is useful for synthesizing cyclic products. Using a newly developed convertible isocyanide, known as indole isocyanide, in the Ugi reaction allowed for the mild synthesis of various pyroglutamic acids. This effort led first to a racemic total synthesis of the natural product dysibetaine. A project to achieve the stereoselective synthesis of the same natural product led to the discovery of a unique Ugi reaction. Usually a carboxylic acid is one of the four reacting components in this reaction, however in this unusual case an ester acts as the carboxylic acid component. In addition to the natural product syntheses, a detailed explanation of the scope and mechanism of the new convertible indole isocyanide is presented. Finally, we reveal a new stereoselective, Brønsted-acid catalyzed Passerini-type reaction.