Pharmaceutical Book from C.H.I.P.S.

Chirality in Drug Research
edited by Eric Francotte

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


  • 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


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


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Chirality in Drug Research
edited by Eric Francotte
2006 • 370 pages • $199.00 + shipping
Texas residents please add 6.75 % sales tax

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