摘要: Preface. List of Contributors. Introduction. 1 Chiral Drugs from a Historical Point View (Joseph Gal). 1.1 1.2 A Word About Words. 1.3 Old Drugs: Natural Remedies 3000BC-1900. 1.4 Recognition Chirality in Drugs. 1.5 Enantioselectivity Drug Action and Metabolism: The Beginnings. 1.6 the 20th Century. References. Synthesis. 2 Stereoselective Synthesis - An Industrial Perspective (Hans-Jurgen Federsel). 2.1 Introduction: Overview. 2.2 Asymmetry an Scale Perspective. 2.3 Processes Manufacture Drivers Blockers. 2.4 Metal Friend Foe. 2.5 Ligand Development At Core Catalytic Chemistry. 2.6 Asymmetric Reactions Rich Reservoir. 2.7 Retrospect Prospect. 3 Aspects Products Discovery (Philipp Krastel, Frank Petersen, Silvio Roggo, Esther Schmitt, Ansgar Schuffenhauer). 3.1 3.2 Stereochemical Products. 3.3 Mechanisms Control Product Biosynthesis. 3.4 Biological Activity Related to Stereochemistry. 4 Biotransformation Methods for Preparing Intermediates (Michael Muller Marcel Wubbolts). 4.1 4.2 Examples Established Applications Biocatalysts Pharmaceuticals. 4.3 Some Special Biocatalysts, Recent Developments. 4.4 Conclusions Outlook. Separations. 5 Resolution by Crystallisation (Kazuhiko Saigo). 5.1 5.2 Physical Enantioseparation Preferential Crystallization. 5.3 Chemical Diastereomeric Salt Formation. 5.4 Bridge Between Crystallization 5.5 Process Research on Racemates 5.6 Enantioseparations Pharmaceutical Industry. 6 Isolation Production Optically Pure Enantioselective Chromatography (Eric Francotte). 6.1 6.2 General Considerations Regarding Preparation Single Stereoisomers 6.3 Preparative Stationary Phases. 6.4 Strategies Performing 6.5 6.6 Conclusion. 7 Chromatographic Analysis (Norbert M. Maier Wolfgang Lindner). 7.1 7.2 Role Development. 7.3 Separation Techniques Enantiomer Analysis. 7.4 Principle Separation. 7.5 Molecular Requirements Recognition. 7.6 Thermodynamic Principles 7.7 Mobile Phase 7.8 Selectors Phases Employed Liquid 7.9 Conclusions. 8 Capillary Electrophoresis Coupled Mass Spectrometry (Serge Rudaz Jean-Luc Veuthey). 8.1 8.2 (CE). 8.3 CE-MS Coupling. 8.4 Strategies. 8.5 Partial Filling. 8.6 Filling Counter Current Technique. 8.7 Micellar Electrokinetic Chromatography. 8.8 Quantitative Parameters CE-ESI-MS 8.9 Electrochromatography Spectrometry. 8.10 Discussion 9 Powerful Tools Enantiopure Alcohols Simultaneous Determination Their Absolute Configurations X-Ray Crystallography and/or 1H NMR Anisotropy (Nobuyuki Harada). 9.1 9.2 Methodologies Determining Configuration. 9.3 CSDP Acid, Camphorsultam Dichlorophthalic Acid (-)-1, Useful Enantioresolution HPLC X-ray 287 9.4 Novel Tool, 2-Methoxy-2-(1-naphthyl)propionic (MalphaNP (S)-(+)-3), Aisotropy Method. 9.5 Configuration Thyroid Hormone Analog KAT-2003 as Determined Method with MalphaNP Acid. 9.6 10 Keywords Modeling Software Literature Modeling, Docking, Ligand-Receptor Interaction Symmetry (Gerd Folkers, Mine Yarim, Pavel Pospisil). 10.1 10.2 QSAR. 10.3 10.4 Protein Residues, Homology Modeling. 10.5 Selective Binding, MDS methods. 10.6 Docking Compounds. 10.7 Dealing References Its Successful Application. Subject Index.
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