Lays the groundwork for developing promising new drug candidates
Drawing 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 hydrogenation
Both 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.
About the Authors xi
1 Transition Metal Catalysis in the Pharmaceutical Industry 1Carl 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 25Hong C. Shen (Roche)
3 Selected Applications of Pd– and Cu–Catalyzed Carbon Heteroatom Cross–Coupling Reactions in the Pharmaceutical Industry 97Jingjun Yin (Merck)
4 Asymmetric Cross–Coupling Reactions 165Vince Yeh (Novartis) and William A. Szabo (Consultant in Drug Development)
5 Metathesis Reactions 215Oliver R. Thiel (Amgen)
6 Transition Metal–Catalyzed Synthesis of Five– and Six–Membered Heterocycles 257Cheol K. Chung (Merck) and Matthew L. Crawley (Main Line Health)
7 Oxidative Catalysis 277Lamont Terrell (GlaxoSmithKline)
8 Industrial Asymmetric Hydrogenation 315Hans–Ulrich Blaser (Solvias)