Part I: Greener Approaches to Classical Transformations
1. Green Synthesis of Common Heterocycles
Christian Schäfer, Hyejin Cho, and Béla Török
2. Greener Methods for Amide Bond Synthesis
Nathan J. Oldenhuis, Aaron M. Whittaker, and Vy M. Dong
3. Mitsunobu Reactions in Medicinal Chemistry and Development of Practical Modifications
Tsuyoshi Taniguchi
4. Direct Nucleophilic Substitution of Alcohols by Brønsted or Lewis Acids Activation: An Update
Pier Giorgio Cozzi, Andrea Gualandi, Luca Mengozzi, Elisabetta Manoni, and Claire Margaret Wilson
5. Friedel-Crafts Reactions
Grigoriy Sereda
6. Ionic Liquids: Design and Applications
Arturo Obregón-Zúñiga and Eusebio Juaristi
Part II: Synthetic Strategy
7. Designing Efficient Cascade Reactions in Drug Discovery
Chenguang Yu, He Huang, Chunquan Sheng, and Wei Wang
8. Multicomponent Synthesis: Cohesive Integration of Green Chemistry Principles
Razvan Cioc, Eelco Ruijter, and Romano V.A. Orru
9. Direct C–H Functionalization Approaches to Pharmaceutically Relevant Molecules
James J. Mousseau and Antonia F. Stepan
10. C–H Activation with Photoredox Catalysis
Joel W. Beatty and Corey R.J. Stephenson
11. In Situ Protecting Groups for Chemoselective Transformations
Alan Steven
Part III: Enabling Technologies
12. Expanding the Biocatalysis Toolbox
Rajesh Kumar, Carlos A. Martinez, and John W. Wong
13. New Directions in Coupling Chemistry
Gary M. Gallego, Rebecca A. Gallego, and Paul F. Richardson
14. Flow Chemistry as an Enabling Technology for Synthetic Organic Chemistry
Nicholas E. Leadbeater
15. Reaction Optimization: A High-Throughput Experimentation Approach
Simon Berritt and Jason R. Schmink
16. Radiopharmaceutical Discovery with 11CO2-Fixation Methods Inspired by Green Chemistry
Benjamin H. Rotstein and Neil Vasdev
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This detailed book highlights several emerging areas in the implementation of green chemistry in medicinal chemistry drug discovery with a specific focus on their application to the expeditious discovery of new biologically active entities. Divided into three sections, the collection explores greener approaches to chemical transformations that are both prevalent and have been highlighted as challenging within the pharmaceutical industry, overall synthetic strategy, as well as the implementation and impact of a range of enabling technologies within medicinal chemistry. As a volume of the Methods in Pharmacology and Toxicology series, chapters provide the kind of key insight that can guide researchers toward greater success in the lab.
Authoritative and practical, Green Chemistry in Drug Discovery: From Academia to Industry provides both a fundamental insight into the progress that has been made as well as some of the challenges that still exist for these techniques to be effectively implemented in the drug discovery process in a routine manner.