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Issue 36, 2016
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Fluorination methods in drug discovery

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Fluorination reactions of medicinal and biologically-active compounds will be discussed. Late stage fluorination strategies of medicinal targets have recently attracted considerable attention on account of the influence that a fluorine atom can impart to targets of medicinal importance, such as modulation of lipophilicity, electronegativity, basicity and bioavailability, the latter as a consequence of membrane permeability. Therefore, the recourse to late-stage fluorine substitution on compounds with already known and relevant biological activity can provide the pharmaceutical industry with new leads with improved medicinal properties. The fluorination strategies will take into account different fluorinating reagents, either of nucleophilic or electrophilic, and of radical nature. Diverse families of organic compounds such as (hetero)aromatic rings, and aliphatic substrates (sp3, sp2, and sp carbon atoms) will be studied in late-stage fluorination reaction strategies.

Graphical abstract: Fluorination methods in drug discovery

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Article information

10 Apr 2016
02 Aug 2016
First published
03 Aug 2016

Org. Biomol. Chem., 2016,14, 8398-8427
Article type
Review Article

Fluorination methods in drug discovery

D. E. Yerien, S. Bonesi and A. Postigo, Org. Biomol. Chem., 2016, 14, 8398
DOI: 10.1039/C6OB00764C

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