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Tailored to the needs of medicinal and natural products chemists, the second edition of this unique handbook brings the contents up to speed,almost doubling the amount of chemical information with an additional volume.As in the predecessor, a short introductory section covers the theoretical background and evaluates currently available instrumentation andequipment. The main part of the book then goes on to systematically survey the complete range of published microwave-assisted synthesismethods from their beginnings in the 1990s to mid-2011, drawing on data from more than 5,000 reports and publications. Throughout, thefocus is on those reactions, reagents and reaction conditions that work, and that are the most relevant for medicinal and natural productschemistry. A much expanded section is devoted to combinatorial, highthroughput and flow chemistry methods.
List of contents
PPREFACEINTRODUCTION: MICROWAVE SYNTHESIS IN PERSPECTIVEMicrowave Synthesis and Medicinal ChemistryMicrowave-Assisted Organic Synthesis (MAOS): A Brief History Scope and Organization of the BookMICROWAVE THEORYMicrowave RadiationMicrowave Dielectric HeatingDielectric PropertiesMicrowave versus Conventional Thermal HeatingMicrowave EffectsEQUIPMENT REVIEWIntroductionDomestic Microwave OvensDedicated Microwave Reactors for Organic SynthesisSingle-Mode InstrumentsMultimode InstrumentsMICROWAVE PROCESSING TECHNIQUESSolvent-Free ReactionsPhase-Transfer CatalysisOpen- versus Closed-Vessel ConditionsPre-pressurized Reaction VesselsNonclassical SolventsPassive Heating ElementsProcessing Techniques in Drug Discovery and High-Throughput SynthesisScale-Up in Batch and Continuous FlowLITERATURE SURVEY PART A: TRANSITION METAL-CATALYZED REACTIONSGeneral CommentsCarbon?Carbon Bond FormationsCarbon?Heteroatom Bond FormationsOther Transition Metal-Mediated ProcessesLITERATURE SURVEY PART B: MISCELLANEOUS ORGANICTransformationsRearrangement ReactionsCycloaddition ReactionsOxidationsReductions and HydrogenationsMitsunobu ReactionsGlycosylation Reactions and Related Carbohydrate-Based TransformationsOrganocatalytic TransformationsOrganometallic Transformations (Mg, Zn, and Ti)Multicomponent ReactionsAlkylation ReactionsNucleophilic Aromatic SubstitutionsRing-Opening ReactionsAddition and Elimination ReactionsSubstitution ReactionsEnamine and Imine FormationsReductive AminationsEster and Amide FormationDecarboxylation ReactionsFree Radical ReactionsProtection/Deprotection ChemistryPreparation of Isotopically Labeled CompoundsMiscellaneous Transformations7 LITERATURE SURVEY PART C: HETEROCYCLE SYNTHESISThree-Membered Heterocycles with One HeteroatomFour-Membered Heterocycles with One HeteroatomFive-Membered Heterocycles with One HeteroatomFive-Membered Heterocycles with Two HeteroatomsFive-Membered Heterocycles with Three HeteroatomsFive-Membered Heterocycles with Four HeteroatomsSix-Membered Heterocycles with One HeteroatomSix-Membered Heterocycles with Two HeteroatomsSix-Membered Heterocycles with Three HeteroatomsLarger Heterocyclic and Polycyclic Ring SystemsLITERATURE SURVEY PART D: COMBINATORIAL CHEMISTRY AND HIGH-THROUGHPUT ORGANIC SYNTHESISSolid-Phase Organic SynthesisSoluble Polymer-Supported SynthesisFluorous-Phase Organic SynthesisGrafted Ionic Liquid-Phase-Supported SynthesisPolymer-Supported ReagentsPolymer-Supported CatalystsPolymer-Supported Scavengers
About the author
Hugo Kubinyi gehört seit 1985 der BASF AG an, wo Kombinatorische Chemie, Molecular Modelling und Wirkstoffdesign zu seinen Tätigkeitsfeldern zählten. Sein Spezialgebiet sind Struktur-Wirkungs-Beziehungen und QSAR-Methoden.
Gerd Folkers is professor of pharmaceutical chemistry at the ETH Zürich since 1991. He studied pharmacy at the University of Bonn and earned his Ph.D. on structure-activity relationships of desapurines. He then moved to the University of Tübingen, where he completed his habilitation in pharmaceutical chemistry. During a stay with H.-D. Hoeltje in Bern, he studied new research methods in computer-aided molecular design and expanded this knowledge during other stays with T. Blundell at the Birkbeck College and E. Meyer at Texas A&M University.The focus of his research is the molecular interaction between drugs and their binding sites. Besides his work on the molecular mechanism of "conventional" nucleoside therapeutics against virus infections and cancer, his special interest has shifted to immuno-therapeutics.
Summary
Tailored to the needs of medicinal and natural products chemists, the second edition of this unique handbook brings the contents up to speed,
almost doubling the amount of chemical information with an additional volume.
As in the predecessor, a short introductory section covers the theoretical background and evaluates currently available instrumentation and
equipment. The main part of the book then goes on to systematically survey the complete range of published microwave-assisted synthesis
methods from their beginnings in the 1990s to mid-2011, drawing on data from more than 5,000 reports and publications. Throughout, the
focus is on those reactions, reagents and reaction conditions that work, and that are the most relevant for medicinal and natural products
chemistry. A much expanded section is devoted to combinatorial, highthroughput and flow chemistry methods.