3rd Edition. – Informa Healthcare, UK, 2012. – 332 p. – ISBN: 1420092383.
Drug Stereochemistry: Analytical Methods and Pharmacology, Third Edition covers all aspects of chiral drugs from academic, governmental, industrial, and clinical perspectives, reflecting the many advances in techniques and methodology. The book provides a solid background on stereochemistry, from its early history, including an overview of terms and concepts, to the current drug development process, legal and regulatory issues, and the new stereoisomeric drugs. It is a one-stop reference for pharmaceutical scientists and chemists working with chiral drug molecules.
The early history of stereochemistry: From the discovery of molecular asymmetry and the first resolution of a racemate by Pasteur to the asymmetrical chiral carbon of van’t Hoff and Le Bel.
Stereochemistry — basic terms and concepts.
Molecular basis of chiral recognition.
The Separation, Preparation, and Identification of Stereochemically Pure Drugs.
Separation and resolution of enantiomers and their dissociable diastereomers through direct crystallization.
Indirect methods for the chromatographic resolution of drug enantiomers.
HPLC chiral stationary phases for the stereochemical resolution of enantiomeric compounds: The current state of the art.
Preparative and production scale chromatography in enantiomer separations.
Enantioselective separations by electromigration techniques.
Alternative analytical techniques for determination or isolation of drug enantiomers.
Pharmacokinetic and Pharmacodynamic Differences Between Drug Stereoisomers.
Stereoselective transport of drugs.
Enantioselective binding of drugs to plasma proteins.
Clinical pharmacokinetics and pharmacodynamics of stereoisomeric drugs.
Perspectives on the Development and Use of Single Isomer Drugs.
Regulatory perspective on the development of new stereoisomeric drugs.
Molecular analysis of agonist stereoisomers at b2-adrenoceptors.
Development of chiral drugs from a U.S. legal patentability perspective: Enantiomers and racemates.
The importance of chiral separations in single enantiomer patent cases.