Jump to main content
Jump to site search

Issue 36, 2016

Fluorination methods in drug discovery

Author affiliations

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

Article information


Submitted
10 Apr 2016
Accepted
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

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.


Social activity

Search articles by author

Spotlight

Advertisements