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二氟甲基化反應研究進展

New Progress in Difluoromethylation

  • 摘要: 由於向有機化合物中引入氟原子或含氟官能團會引起其理化性質🦹🏻、生物活性等性能的顯著改變或提升🤛🏿,而且有機氟化合物在醫藥、農藥和新材料等方面發揮著不可或缺的作用,因此開發各類有機氟化反應具有重要的學術和應用價值。其中,向分子中引入二氟甲基是氟化學的熱門研究領域。近年來,各類二氟甲基化試劑以高效、安全、經濟的優點應用於二氟甲基化反應中。本文將各類二氟甲基化反應根據其使用的不同二氟甲基化試劑分為含氟甲烷類🤟🏽、TMS類、含氟羧酸及羧酸衍生物類、含氟磷酸酯、含氟碸類🧔🏼‍♀️、二氟甲基金屬試劑以及其他類🫢,較為詳細地介紹了近五年來報道的烷烴、芳烴、雜原子等的直接🧍🏻‍♂️、自由基、卡賓等機製的二氟甲基化反應研究。

     

    Abstract: Organic fluorine compounds played an indispensable role in medicines, pesticides and new materials due to the introduction of fluorine atoms or fluorine groups into organic compounds, which brought about significant changes or enhancements in their physical and chemical properties, biological activities and other properties. Therefore, the development of various types of organic fluorination reactions had important academic and application value. Among them, the introduction of difluoromethyl groups into molecules was a hot research field in fluorine chemistry.In recent years, various difluoromethylation reagents have been used in difluoromethylation reactions with the advantages of high efficiency, safety and economy. In this paper, the difluoromethylation reaction was divided as fluorinated methane, TMS, fluorine-containing carboxylic acid and carboxylic acid derivatives, fluorine-containing phosphates, fluorine-containing sulfones, difluoromethyl metal reagents, and other types. The direct, radical and Valery Karpin difluoromethylation of alkanes, aromatics and heteroatoms reported in the past five years were reviewed in detail.

     

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