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Informationen zum Autor MATTHEW L. CRAWLEY, PHD, is the Director of the Community Physician Electronic Medical Records Program at Main Line Health. Previously, he has worked as a medicinal chemist at Pfizer and Wyeth Research. Dr. Crawley is an author of more than twenty publications, and his discoveries have resulted in several patents. BARRY M. TROST, PHD, is Tamaki Professor of Humanities and Sciences in the Department of Chemistry at Stanford University. Dr. Trost has been elected a Fellow of the American Academy of Sciences and member of the National Academy of Sciences. He has served as chairman of the NIH Medicinal Chemistry Study Section, held over 120 university lectureships, and presented over 260 plenary lectures at national and international meetings. Klappentext Lays the groundwork for developing promising new drug candidatesDrawing on real-life examples, this book demonstrates the applications of transition metal catalysis in drug discovery and development, and its role in the efficient creation of both preclinical and clinical drug candidates as well as commercialized drugs. The authors pay particular attention to the challenges of transitioning reactions developed in academic labs into scalable industrial processes.Applications of Transition Metal Catalysis in Drug Discovery and Development begins with a general overview of the use of transition metal catalysis in the pharmaceutical industry. Next, it covers:* Transition metal-catalyzed carbon-carbon cross-coupling reactions* Palladium- and copper-catalyzed carbon-heteroatom cross-coupling reactions* Asymmetric cross-coupling reactions and metathesis* Transition metal-catalyzed synthesis of five- and six-membered heterocycles* Oxidative catalysis and industrial asymmetric hydrogenationBoth the editors and authors are internationally recognized experts in drug discovery and development. All authors are scientists from such major pharmaceutical companies as Boehringer Ingelheim, GlaxoSmithKline, Merck, Amgen, and Novartis. Additionally, many of the authors have been responsible for developing the reactions and the drugs discussed in the book, providing readers with firsthand accounts of their discoveries.This remarkable work serves as a guide, historical perspective, and practical compendium, offering pharmaceutical researchers and medicinal chemists a unique perspective on the applications of transition metal catalysis in drug discovery and development. Moreover, the book lays the groundwork for continued development of transition metal-catalyzed processes, setting the stage for new and promising drug candidates. Zusammenfassung This book documents examples of transition metal catalysis in drug discovery and development from an industrial perspective. Co-edited by Barry Trost, one of the foremost organic research chemists, the authors pay particular attention to transitioning academically-developed reactions into scalable industrial processes. Inhaltsverzeichnis Preface vii Contributors ix About the Authors xi 1 Transition Metal Catalysis in the Pharmaceutical Industry 1 Carl A. Busacca, Daniel R. Fandrick, Jinhua J. Song, and Chris H. Senanayake (Boehringer Ingelheim Pharmaceuticals) 2 Selected Applications of Transition Metal-Catalyzed Carbon-Carbon Cross-Coupling Reactions in the Pharmaceutical Industry 25 Hong C. Shen (Roche) 3 Selected Applications of Pd- and Cu-Catalyzed Carbon-Heteroatom Cross-Coupling Reactions in the Pharmaceutical Industry 97 Jingjun Yin (Merck) 4 Asymmetric Cross-Coupling Reactions 165 Vince Yeh (Novartis) and William A. Szabo (Consultant in Drug Development) 5 Metathesis Reactions 215 Oliver R. Thiel (Amgen) 6 Transition Metal-Catalyzed Synthesis of Five- and Six-Membered Heterocycles 257 Cheol K. Chung (Merck) and Matthew L. Crawley (M...
List of contents
Preface vii
Contributors ix
About the Authors xi
1 Transition Metal Catalysis in the Pharmaceutical Industry 1
Carl A. Busacca, Daniel R. Fandrick, Jinhua J. Song, and Chris H. Senanayake (Boehringer Ingelheim Pharmaceuticals)
2 Selected Applications of Transition Metal-Catalyzed Carbon-Carbon Cross-Coupling Reactions in the Pharmaceutical Industry 25
Hong C. Shen (Roche)
3 Selected Applications of Pd- and Cu-Catalyzed Carbon-Heteroatom Cross-Coupling Reactions in the Pharmaceutical Industry 97
Jingjun Yin (Merck)
4 Asymmetric Cross-Coupling Reactions 165
Vince Yeh (Novartis) and William A. Szabo (Consultant in Drug Development)
5 Metathesis Reactions 215
Oliver R. Thiel (Amgen)
6 Transition Metal-Catalyzed Synthesis of Five- and Six-Membered Heterocycles 257
Cheol K. Chung (Merck) and Matthew L. Crawley (Main Line Health)
7 Oxidative Catalysis 277
Lamont Terrell (GlaxoSmithKline)
8 Industrial Asymmetric Hydrogenation 315
Hans-Ulrich Blaser (Solvias)
Index 343
Report
"The book will be particularly appreciated by young scientists, especially those aspiring to a future in the pharmaceutical industry, because it shows what kind of problems they will be asked to solve once they start their industrial career." (ChemMedChem, 1 March 2013)
"All chapters are well-written and comprehensive with lots of examples from OPR and D. The book is highly recommended to all process chemists." (Organic Process Research & Development Journal, 1 November 2012)
