Fluorination methods in drug discovery

Organic & Biomolecular Chemistry Pub Date: 2016-08-03 DOI: 10.1039/C6OB00764C

Abstract

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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