二氟卡宾试剂在有机合成中的应用研究进展

Research Progress on the Application of Difluorocarbene Reagents in Organic Synthesis

氟作为最强电负性的非金属元素,将其引入到有机分子中能赋予分子独特的物理化学性质。含氟及三氟甲基(CF3)的分子在药物化学领域已被广泛研究应用,近年来,含二氟甲基(CHF2)的分子也日益受到关注。研究显示,二氟甲基基团的引入不仅能增强药物的生物活性、改善其溶解度和生物可利用性,还能优化代谢稳定性和细胞膜透过性,降低毒性。本文总结了近年来二氟卡宾试剂在C-二氟甲基化、N-二氟甲基化、O-二氟甲基化以及S-二氟甲基化等反应中的应用。

Fluorine, as the most electronegative non-metal element, imparts unique physicochemical properties to organic molecules when introduced into them. Molecules containing fluorine and trifluoromethyl (CF3) have been extensively studied and applied in the field of medicinal chemistry. In recent years, molecules containing difluoromethyl (CHF2) groups have also attracted increasing attention. Studies have shown that the introduction of difluoromethyl groups can not only enhance the biological activity of drugs, improve their solubility and bioavailability, but also optimize metabolic stability and cell membrane permeability, and reduce toxicity. This article summarizes the applications of difluorocarbene reagents in C-difluoromethylation, N-difluoromethylation, O-dif- luoromethylation, and S-difluoromethylation reactions in recent years.