INVESTIGADORES
POSTIGO Jose Alberto
artículos
Título:
FLUORINATION METHODS IN DRUG DISCOVERY
Autor/es:
DAMIÁN YERIEN; BONESI, SERGIO M.; AL POSTIGO
Revista:
ORGANIC & BIOMOLECULAR CHEMISTRY
Editorial:
ROYAL SOC CHEMISTRY
Referencias:
Lugar: CAMBRIDGE-DOI: 10.1039/C6OB00764C; Año: 2016 vol. 14 p. 8398 - 8427
ISSN:
1477-0520
Resumen:
DOI: 10.1039/C6OB00764CFluorination 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 the fluorine atom can impart to targets of medicinal importance, such as a modulation of lipophilicity, electronegativity, basicity and bioavailability, this 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, nucleophilic, 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.
