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Full Description
Presents state-of-the-art strategies for the late-stage functionalization and diversity-oriented synthesis of challenging organic compounds
Late-stage functionalization (LSF) and diversity-oriented synthesis have emerged as powerful approaches in contemporary organic chemistry, enabling the selective modification of complex molecules at advanced stages of synthesis. These strategies offer unique advantages in drug discovery, medicinal chemistry, and natural product derivatization, where access to structurally diverse analogues is crucial. By allowing transformations that would otherwise require lengthy synthetic routes, LSF and diversity-oriented synthesis open pathways to molecules of high biological, pharmaceutical, and material relevance, significantly streamlining discovery processes.
Late-Stage Functionalization and Diversification in Organic Synthesis: Methods and Applications provides a comprehensive overview of the latest developments in this rapidly expanding field. Presenting both practical methodologies and mechanistic insights, the book covers transition metal catalysis, photo- and electrocatalysis, flow chemistry, and radioisotope insertion. In addition, the book:
Places a unique focus on diversity-oriented synthesis, showcasing C-O, C-N, and C-S bond activation
Highlights molecular editing and stereochemical editing as powerful new strategies for structural diversification
Includes applications to natural products, pharmaceuticals, and radiopharmaceuticals
Late-Stage Functionalization and Diversification in Organic Synthesis: Methods and Applications is essential reading for graduate students, postdoctoral researchers, and professionals in organic chemistry, medicinal chemistry, and natural products research. It is particularly suited for advanced courses in organic synthesis and catalysis, and also serves as a practical reference for chemists working in the pharmaceutical and biotechnology industries.
Contents
PART 1: C-H FUNCTIONALIZATION
1. Transition-metal Catalyzed C-H Activation
2. HAT processes
3. Photocatalysis
4. Electrocatalysis
5. Flow chemistry
PART 2: C-X FUNCTIONALIZATION
6. C-O (ester, ether)
7. C-N (amide)
8. C-S (thiols)
PART 3: LATE-STAGE CROSS-COUPLING REACTIONS
9. Suzuki-Miyaura Cross-coupling Reactions
10. Cross-coupling Amination Late-stage Transformations
PART 4: LATE-STAGE FORMATION OF A C-Rf Bond
11. C-F and C-CF3 Bonds
12. C-Rf Groups
13. 18F Groups
PART 5: MISCELLANEOUS
14. Chemoselective Functionalization
15. Biocatalysis approaches
16. Molecular/stereochemical Editing
17. Synopses Focused on Natural products, and Drug Discovery
