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Divided into the three main sections of synthesis, analysis and drug development, this handbook covers all stages of the drug development process, including large-scale synthesis and purification of chirally pure pharmaceuticals.
The two editors from academia and a major pharmaceutical company have assembled an experienced, international team who provide first-hand practical advice and report previously unpublished data.
In the first section, the isolation of chiral drugs from natural sources, their production in enzymatic processes and the resolution of racemic mixtures in preparative chromatography are outlined in separate chapters. For the section on qualitative and quantitative analysis, enantioselective chromatographic methods are presented as well as optical methods and CE-MS, while the final section deals with the pharmacology, pharmacokinetics and metabolic aspects of chiral drugs, devoting whole chapters to stereoselective drug binding and modeling chiral drug-receptor interactions.
With its unique industry-relevant aspects, this is a must for medicinal and pharmaceutical chemists.
List of contents
INTRODUCTION
Chiral drugs from a historical point of view (J. Gal)
SYNTHESIS
Stereoselective synthesis of chiral drugs (H. Federsel)
Chiral drugs from natural source (F. Petersen)
Biotransformation methods for preparing chiral drugs and drug intermediates (M. Müller, M. Wubbolts)
SEPARATIONS
Resolution of chiral drugs and drug intermediates by crystallisation (K. Saigo)
Resolution of chiral drugs by preparative chromatography (E. Francotte)
ANALYSIS
Stereoselective chromatographic methods for drug analysis (W. Lindner)
CE-MS for the quantitative analysis of chiral drugs (J. Veuthey)
Spectrosopic methods for chiral drug analysis (N. Harada)
Modeling of chiral drug-receptor interactions (G. Folkers)
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
Divided into the three main sections of synthesis, analysis and drug development, this handbook covers all stages of the drug development process, including large-scale synthesis and purification of chirally pure pharmaceuticals.
The two editors from academia and a major pharmaceutical company have assembled an experienced, international team who provide first-hand practical advice and report previously unpublished data.
In the first section, the isolation of chiral drugs from natural sources, their production in enzymatic processes and the resolution of racemic mixtures in preparative chromatography are outlined in separate chapters. For the section on qualitative and quantitative analysis, enantioselective chromatographic methods are presented as well as optical methods and CE-MS, while the final section deals with the pharmacology, pharmacokinetics and metabolic aspects of chiral drugs, devoting whole chapters to stereoselective drug binding and modeling chiral drug-receptor interactions.
With its unique industry-relevant aspects, this is a must for medicinal and pharmaceutical chemists.
Additional text
"... In general, the book has been welledited and produced and contains a useful subject index."
ChemMedChem
"...As appropriately stressed throughout the book, the several issues associated with chirality have emerged as major factors in drug design and development. This book is a timely and well written resource."
Journal of Medicinal Chemistry, 06/2007
"...Overall this is a useful book for process chemists working with chiral compounds in industry and the chapters highlighted in this review are recommended reading."
Organic Process Research and Development Journal, 08/2007
Report
"... In general, the book has been welledited and produced and contains a useful subject index."
ChemMedChem
"...As appropriately stressed throughout the book, the several issues associated with chirality have emerged as major factors in drug design and development. This book is a timely and well written resource."
Journal of Medicinal Chemistry, 06/2007
"...Overall this is a useful book for process chemists working with chiral compounds in industry and the chapters highlighted in this review are recommended reading."
Organic Process Research and Development Journal, 08/2007
