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含氟基团拥有强吸电子性和高亲脂性,有机分子适当地引入含氟基团可以改善其原有的功能.因此,向分子内引入含氟基团的方法成为了当前的研究热点.由于三氟甲硫基拥有突出的性能,其引入方法成为主要研究热点之一,三氟甲硒基、三氟甲氧基以及三氟乙氧基的引入方法也受到了科研人员的关注.~(18)F拥有几乎理想的原子核性能,是临床成像使用最广泛的正电子发射断层显像(PET)放射性核素.因此,新型[~(18)F]放射性示踪剂的研发成为很多科研人员的研究方向.研发新型[~(18)F]放射性示踪剂的关键在于用~(18)F对生物分子进行标记.介绍了最近报道的向分子内直接引入CF_3X(X=S,Se,O,CH_2O)基团的新方法以及一些~(18)F-标记方法的研究成果.此外,总结了一些该领域值得关注的研究方向.
Fluorine-containing groups have strong electron-withdrawing properties and high lipophilicity, and proper introduction of fluorine-containing groups by organic molecules can improve their original functions. Therefore, the introduction of fluorine-containing groups into molecules has become the current research hotspot. Due to the outstanding performance of trifluoromethylthio, its introduction method has become one of the main research hotspots. The introduction of trifluoro-methylselenyl, trifluoromethoxy and trifluoroethoxy has also attracted the attention of researchers. (18) F possesses almost ideal nucleus properties and is the most widely used positron emission tomography (PET) radionuclide for clinical imaging. Therefore, the research and development of novel [~ (18) F] The key to the development of new [~ (18) F] radiotracers lies in the labeling of biomolecules with ~ (18) F. A recently introduced direct introduction of CF_3X (X = S, Se , O, CH_2O) groups as well as the results of some ~ (18) F-labeling methods.In addition, some research directions worthy of attention in this field are summarized.