This book focuses on the drug discovery and development
applications of transition metal catalyzed processes, which can
efficiently create preclinical and clinical drug candidates as well
as marketed drugs. The authors pay particular attention to
the challenges of transitioning academically-developed reactions
into scalable industrial processes. Additionally, the book lays the
groundwork for how continued development of transition metal
catalyzed processes can deliver new drug candidates. This work
provides a unique perspective on the applications of transition
metal catalysis in drug discovery and development – it is a
guide, a historical prospective, a practical compendium, and a
source of future direction for the field.
Daftar Isi
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 (Glaxo Smith Kline)
8 Industrial Asymmetric Hydrogenation 315
Hans-Ulrich Blaser (Solvias)
Index 243
Tentang Penulis
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.
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