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      China's flourishing synthetic organofluorine chemistry: innovations in the new millennium

      , ,
      National Science Review
      Oxford University Press (OUP)

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          Abstract

          The new millennium has witnessed the rapid development of synthetic organofluorine chemistry all over the world, and chemists in China have made significant contributions in this field. This review aims to provide a brief introduction to China's primary innovations from 2000 to early 2017, covering fluorination, fluoroalkylation, fluoromethylthiolation, fluoroolefination and polyfluoroarylation, as well as synthesis with fluorinated building blocks. Recent advances in the chemistry of difluorocarbene and the chemistry of carbon–fluorine bond activation are also discussed. As a conclusion, the review ends with some personal perspectives on the future development of China's synthetic organofluorine chemistry.

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          Fluorine in medicinal chemistry.

          It has become evident that fluorinated compounds have a remarkable record in medicinal chemistry and will play a continuing role in providing lead compounds for therapeutic applications. This tutorial review provides a sampling of renowned fluorinated drugs and their mode of action with a discussion clarifying the role and impact of fluorine substitution on drug potency.
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            Introduction of fluorine and fluorine-containing functional groups.

            Over the past decade, the most significant, conceptual advances in the field of fluorination were enabled most prominently by organo- and transition-metal catalysis. The most challenging transformation remains the formation of the parent C-F bond, primarily as a consequence of the high hydration energy of fluoride, strong metal-fluorine bonds, and highly polarized bonds to fluorine. Most fluorination reactions still lack generality, predictability, and cost-efficiency. Despite all current limitations, modern fluorination methods have made fluorinated molecules more readily available than ever before and have begun to have an impact on research areas that do not require large amounts of material, such as drug discovery and positron emission tomography. This Review gives a brief summary of conventional fluorination reactions, including those reactions that introduce fluorinated functional groups, and focuses on modern developments in the field. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
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              Electrophilic trifluoromethylation by use of hypervalent iodine reagents.

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                Author and article information

                Journal
                National Science Review
                Oxford University Press (OUP)
                2095-5138
                2053-714X
                May 2017
                May 01 2017
                June 06 2017
                May 2017
                May 01 2017
                June 06 2017
                : 4
                : 3
                : 303-325
                Article
                10.1093/nsr/nwx058
                3ce481d3-bb45-4af0-880d-1a98437d7f11
                © 2017

                http://creativecommons.org/licenses/by/4.0/

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