Artículo

Yerien, D.E.; Bonesi, S.; Postigo, A. "Fluorination methods in drug discovery" (2016) Organic and Biomolecular Chemistry. 14(36):8398-8427
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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. © 2014 The Royal Society of Chemistry.

Registro:

Documento: Artículo
Título:Fluorination methods in drug discovery
Autor:Yerien, D.E.; Bonesi, S.; Postigo, A.
Filiación:Departamento de Química Orgánica, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires-CONICET, Junín 954, Buenos Aires, CP 1113, Argentina
Departamento de Química Orgánica, CIHIDECAR-CONICET, Pabellón II, Ciudad Universitaria, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Buenos Aires, 1428, Argentina
Palabras clave:Bioactivity; Biochemistry; Carbon; Chemical bonds; Electronegativity; Fluorination; Halogenation; Aromatic rings; Biologically active compounds; Drug discovery; Fluorination reactions; Fluorine atoms; Fluorine substitution; Membrane permeability; Pharmaceutical industry; Fluorine; fluorinated hydrocarbon; fluorine; chemical structure; chemistry; drug development; halogenation; synthesis; Drug Discovery; Fluorine; Halogenation; Hydrocarbons, Fluorinated; Molecular Structure
Año:2016
Volumen:14
Número:36
Página de inicio:8398
Página de fin:8427
DOI: http://dx.doi.org/10.1039/c6ob00764c
Título revista:Organic and Biomolecular Chemistry
Título revista abreviado:Org. Biomol. Chem.
ISSN:14770520
CODEN:OBCRA
CAS:fluorine, 7782-41-4; Fluorine; Hydrocarbons, Fluorinated
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_14770520_v14_n36_p8398_Yerien

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Citas:

---------- APA ----------
Yerien, D.E., Bonesi, S. & Postigo, A. (2016) . Fluorination methods in drug discovery. Organic and Biomolecular Chemistry, 14(36), 8398-8427.
http://dx.doi.org/10.1039/c6ob00764c
---------- CHICAGO ----------
Yerien, D.E., Bonesi, S., Postigo, A. "Fluorination methods in drug discovery" . Organic and Biomolecular Chemistry 14, no. 36 (2016) : 8398-8427.
http://dx.doi.org/10.1039/c6ob00764c
---------- MLA ----------
Yerien, D.E., Bonesi, S., Postigo, A. "Fluorination methods in drug discovery" . Organic and Biomolecular Chemistry, vol. 14, no. 36, 2016, pp. 8398-8427.
http://dx.doi.org/10.1039/c6ob00764c
---------- VANCOUVER ----------
Yerien, D.E., Bonesi, S., Postigo, A. Fluorination methods in drug discovery. Org. Biomol. Chem. 2016;14(36):8398-8427.
http://dx.doi.org/10.1039/c6ob00764c