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

Fluorination strategies can impact targets of medicinal importance in a range of useful ways, including facilitating modulation of their lipophilicity, electronegativity, basicity and bioavailability. Late Stage Fluorination of Bioactive Molecules reviews how the use of such 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 and those of a radical nature, and diverse families of organic compounds, such as (hetero) aromatic rings and aliphatic substrates.

Drawing on the author’s expert knowledge, this volume provides researchers with a broad set of applicable methods to use in their work, supporting and facilitating the development of novel, enhanced drugs using fluorination strategies.

Highlights the latest developments in the field in one concise volumeProvides details of key fluorinating reagents across diverse families of organic compoundsExplores the current applications and future potential of fluorine in drug development

1. Introduction and Highlights 2. 18F radiolabeling of bioactive compounds 3. Electrophilic and oxidative fluorination of aromatic compounds 4. Enantioselective fluorination 5. Visible-Light-Mediated C-F bond Activation 6. Photocatalytic fluorination reactions 7. Fluorination of allylic positions towards the synthesis of fluorinated bioactive compounds 8. Difluoromethylation of Bioactive Compounds 9. Fluorination of Bioactive Compounds by Electron Transfer Reactions 10. Fluorine-Containing Pharmaceuticals and the Phenomenon of Self-Disproportionation of Enantiomers (SDE)