Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates

Highlights fluorination reactions of medicinal and biologically-active compounds for the discovery and development of new drugs

Al Postigo (Author)

9780128129586, Elsevier Science

Paperback, published 10 September 2018

390 pages
22.9 x 15.1 x 2.5 cm, 0.57 kg

Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates reviews how the use of these techniques on compounds with already known and relevant biological activity can provide new pharmaceutical leads with improved medicinal properties. The fluorination strategies discussed take into account both conventional and novel reagents, including nucleophilic, electrophilic, those of a radical nature, and diverse families of organic compounds, such as (hetero) aromatic rings and aliphatic substrates. Drawing on the authors' expert knowledge, this book provides researchers with a broad set of applicable methods to use in their work.

1. Introduction and Highlights2. 18F radiolabeling of bioactive compounds 3. Electrophilic and oxidative fluorination of aromatic compounds4. Enantioselective fluorination5. Visible-Light-Mediated C-F bond Activation6. Photocatalytic fluorination reactions7. Fluorination of allylic positions towards the synthesis of fluorinated bioactive compounds8. Difluoromethylation of Bioactive Compounds9. Fluorination of Bioactive Compounds by Electron Transfer Reactions10. Fluorine-Containing Pharmaceuticals and the Phenomenon of Self-Disproportionation of Enantiomers (SDE)

Subject Areas: Organic chemistry [PNN]