铜催化氟砜基二氟乙酸甲酯的三氟甲基化反应以及亚磷酸二酯的三氟乙基化反应

发布时间：2018-05-28 21:13

本文选题：三氟甲基化反应 + 催化量　；参考：《上海应用技术大学》2017年硕士论文

【摘要】：由于氟原子能显著地改变母体分子的酸碱性、亲脂性、构象和代谢稳定性,各种含氟基团广泛的出现在药物分子中。随着各种氟化试剂的发展和许多高效的氟化、多氟化反应的发现,含氟化合物被应用于医药、农药、材料领域。本文主要是对铜催化三氟甲基化和三氟乙基化反应的研究。第一部分:铜催化陈氏试剂的三氟甲基化反应。我们利用稳定,廉价的陈氏试剂为三氟甲基化试剂,成功发展了一种新的芳香卤代物的三氟甲基化反应。该反应只需催化量的无水氯化铜催化,以良好的收率得到了一系列三氟甲基化的产物。该反应操作简单、反应时间短、官能团兼容性较好,为陈氏试剂的开发利用提供了一条新的路径。第二部分:以亚磷酸二酯为底物,在铜参与下,以氟氯烷烃HCFC-123为三氟乙基源研究了三氟乙基亚磷酸酯合成放大工艺。为消减或淘汰对臭氧层造成破坏的氟氯烷烃HCFC-123做出了一定的贡献。
[Abstract]:Due to the significant changes in the acidity and alkalinity, lipophilicity, conformation and metabolic stability of the parent molecule, fluorine-containing groups are widely found in the drug molecules. With the development of various fluorinated reagents and the discovery of many efficient fluorination and polyfluorination reactions, fluorinated compounds have been used in medicine, pesticides and materials. In this paper, copper catalyzed trifluoromethylation and trifluoroethylation were studied. Part I: copper catalyzed trifluoromethylation of Chen's reagent. A new trifluoromethylation reaction of aromatic halides was successfully developed by using stable and cheap Chen's reagent as trifluoromethylation reagent. A series of trifluoromethylation products were obtained by using anhydrous copper chloride as catalyst in good yield. The reaction process is simple, the reaction time is short, and the functional group compatibility is good, which provides a new way for the development and utilization of Chen's reagent. The second part: the synthesis and amplification process of trifluoroethyl phosphite was studied with the participation of copper and hydrochlorofluoroalkane hydrocarbon HCFC-123 as trifluoroethyl source. In order to reduce or phase out the ozone layer causing damage to hydrochlorinated hydrocarbon HCFC-123 has made a certain contribution.
【学位授予单位】：上海应用技术大学
【学位级别】：硕士
【学位授予年份】：2017
【分类号】：O621.251

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