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      Copper-Mediated Difluoromethylation of (Hetero)aryl Iodides and β-Styryl Halides with Tributyl(difluoromethyl)stannane

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          Fluorine in pharmaceuticals: looking beyond intuition.

          K. Müller, C. Faeh, F Diederich (2007)
          Fluorine substituents have become a widespread and important drug component, their introduction facilitated by the development of safe and selective fluorinating agents. Organofluorine affects nearly all physical and adsorption, distribution, metabolism, and excretion properties of a lead compound. Its inductive effects are relatively well understood, enhancing bioavailability, for example, by reducing the basicity of neighboring amines. In contrast, exploration of the specific influence of carbon-fluorine single bonds on docking interactions, whether through direct contact with the protein or through stereoelectronic effects on molecular conformation of the drug, has only recently begun. Here, we review experimental progress in this vein and add complementary analysis based on comprehensive searches in the Cambridge Structural Database and the Protein Data Bank.
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            Fluorination in Medicinal Chemistry: Methods, Strategies, and Recent Developments

            Kenneth L Kirk (2008)
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              Organofluorine Chemistry

              Kenji Uneyama (2006)
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                Author and article information

                Journal
                Title: Angewandte Chemie International Edition
                Abbreviated Title: Angew. Chem. Int. Ed.
                Publisher: Wiley-Blackwell
                ISSN: 14337851
                Publication date Created: November 26 2012
                Publication date (Print): November 26 2012
                Volume: 51
                Issue: 48
                Pages: 12090-12094
                Article
                DOI: 10.1002/anie.201205850
                SO-VID: b3f7821e-cf8b-4e50-bcf5-7fd802939398
                Copyright © © 2012
                License:

                http://doi.wiley.com/10.1002/tdm_license_1.1

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