二氟烷基化的研究进展  

Research Progress on Difluoroalkylation

作　　者：王欢欢 郑丁铭 

机构地区：[1]浙江师范大学,化学与生命科学学院,浙江 金华

出　　处：《有机化学研究》2023年第4期182-192,共11页Journal of Organic Chemistry Research

摘　　要：有机氟化合物广泛存在于药物、农用化学品、材料和PET成像应用中。将氟原子或含氟基团掺入药物分子中通常可以改善其生物和物理性质,包括生物利用度、代谢稳定性、亲脂性和结合选择性等。据统计,超过20%的药物分子中含有氟原子,包括最畅销的药物,如立普妥、百忧解和西普贝等。二氟甲基作为含氟基团能使药物分子具有更好的代谢稳定性,因此对化合物二氟烷基化的研究具有重要意义。文献调研后,本文对近年来二氟烷基化的研究进行总结和探讨,尤其对烯烃和炔烃的二氟烷基化进行了详细的介绍。Organofluorine compounds play a central role in a wide range of pharmaceutical, agrochemical, material, and PET imaging applications. The incorporation of fluorine atoms or fluorine-containing groups into organic compounds can often significantly improve biological and physical properties, including bioavailability, metabolic stability, lipophilicity, and binding selectivity. It is estimated that more than 20% of drugs contain at least one fluorine atom, including best-selling drugs such as Lipitor, Prozac, and Cipbe. Difluoromethyl as a fluorinated group can endow drug molecules with better metabolic stability, making the study of the difluoromethylation of compounds significantly important. After a careful literature review, this paper provides a summary and discussion of research on difluoromethylation in recent years, particularly providing a detailed introduction to the difluoromethylation of alkenes and alkynes.

关 键 词：有机氟化合物 二氟烷基化 

分 类 号：R74[医药卫生—神经病学与精神病学]