Chirality in Drug Research covers all stages of the drug development process, including large-scale synthesis and purification of chirally pure pharmaceuticals.

Features:

• Outlines chiral drugs from natural sources, their production in enzymatic processes and the resolution of racemic mixtures in preparative chromatography
• Presents qualitative and quantitative analysis, and enantioselective chromatographic methods

Contents

Chiral Drugs from a Historical Point of View

• AWord About Words
• Old Chiral Drugs: Natural Remedies 3000BC–1900
• Recognition of Chirality in Drugs
• Enantioselectivity in Drug Action and Drug Metabolism: The Beginnings.
• Drug Chirality in the 20th Century

Stereoselective Synthesis of Drugs – An Industrial Perspective

• Asymmetry from an Industrial Scale Perspective
• Stereoselective Processes in Drug Manufacture – Drivers and Blockers
• The Metal – Friend and Foe
• Ligand Development – At the Core of Catalytic Chemistry
• Asymmetric Reactions – A Rich Reservoir

Aspects of Chirality in Natural Products Drug Discovery

• Stereochemical Aspects of Natural Products
• Mechanisms of Stereochemical Control in Natural Product Biosynthesis
• Biological Activity of Natural Products Related to Stereochemistry

Biotransformation Methods for Preparing Chiral Drugs and Drug Intermediates

• Examples of Established Applications of Biocatalysts in the Synthesis of Pharmaceuticals
• Some Special Aspects of Biocatalysts, Recent Developments

Resolution of Chiral Drugs and Drug Intermediates by Crystallisation

• Physical Enantioseparation – Preferential Crystallization
• Chemical Enantioseparation – Diastereomeric Salt Formation
• The Bridge Between Preferential Crystallization and Diastereomeric Salt Formation
• Process Research on the Enantioseparation of Racemates by Diastereomeric Salt Formation
• Examples of Enantioseparations in the Pharmaceutical Industry

Isolation and Production of Optically Pure Drugs by Enantioselective Chromatography

• Preparative Chiral Stationary Phases
• Strategies for Performing Enantioselective Separations
• Preparative Enantioselective Resolution of Chiral Drugs

Stereoselective Chromatographic Methods for Drug Analysis

• The Role of Enantioselective Analysis in Drug Development
• Separation Techniques in Enantiomer Analysis
• Principle of Enantiomer Separation
• Molecular Requirements for Chiral Recognition
• Thermodynamic Principles of Enantiomer Separation
• Role of Mobile Phase in Enantiomer Separation
• Chiral Selectors and Chiral Stationary Phases Employed in Liquid Chromatographic Enantiomer Separation

Capillary Electrophoresis Coupled to Mass Spectrometry for Chiral Drugs Analysis

• Capillary Electrophoresis (CE)
• CE-MS Coupling
• Chiral Separation Strategies
• Partial Filling
• Partial Filling – Counter Current Technique
• Chiral Micellar Electrokinetic Chromatography
• Quantitative Aspects in CE-MS and Parameters for CE-ESI-MS Coupling
• Capillary Electrochromatography Coupled to Mass Spectrometry

Powerful Chiral Molecular Tools for Preparation of Enantiopure Alcohols and Simultaneous Determination of Their Absolute Configurations by X-Ray Crystallography and/or 1H NMR Anisotropy Methods

• Methodologies for Determining Absolute Configuration
• CSDP Acid, Camphorsultam Dichlorophthalic Acid (–)-1, Useful for the Enantioresolution of Alcohols by HPLC and Simultaneous Determination of Their Absolute Configurations by X-ray Crystallography
• A Novel Chiral Molecular Tool, 2-Methoxy-2-(1-naphthyl)propionic Acid (MαNP Acid (S)-(+)-3), Useful for Enantioresolution of Alcohols and Simultaneous Determination of Their Absolute Configurations by the ¹H NMR Aisotropy Method
• Absolute Configuration of the Thyroid Hormone Analog KAT-2003 as Determined by the 1H NMR Anisotropy Method with MαNP Acid

Keywords in Chirality Modeling Molecular Modeling of Chirality – Software and Literature Research on Chirality in Modeling, Chirality in Docking, Chiral Ligand–Receptor Interaction and Symmetry

• Chirality in QSAR
• Molecular Modeling in Chiral Chromatography
• Chirality of Protein Residues, Homology Modeling
• Chiral Selective Binding, MDS methods
• Docking of Chiral Compounds
• Molecular Modeling Software Dealing with Chirality and Some References to Its Successful Application

Index

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