Green Chemistry in Drug Discovery From Academia to Industry

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. 

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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