分子内直接引入含氟基团以及^(18)F-标记方法研究进展  

Recent Advances of Direct Incorporation of Fluorine-Containing Groups and ^(18)F-Labeling Methods

作　　者：李恭铭 孙德群[1] 

机构地区：[1]山东大学(威海)海洋学院,威海264209

出　　处：《有机化学》2016年第8期1715-1740,共26页Chinese Journal of Organic Chemistry

摘　　要：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 effect and high lipophilicity, organic molecules incorporated fluorine-containing groups can improve its function. Therefore, the incorporation of fluorine-containing groups into molecules has become the current research hotspot. The method for incorporation of CF3S group becomes one of the hot research field due to its excellent nature. The strategy for incorporation of CF3Se, CF30 and CF3CH2O groups has also been the attention of researchers, ^18F has nearly ideal nuclear properties and is the most widely used positron emission tomography （PET） radioisotope for clinical imaging. Therefore, the development of new [^18F]radiotracers becomes the research focus of many researchers. The method for ^18F-labeling of biomolecules is the key to the development of new [^18F]radiotracers. This paper mainly introduce the recently reported methodology of direct incorporating CF3X （X=S, Se, O, CH2O） groups into molecules and some research results of ^18F-labeling methods. Furthermore, some noteworthy research directions in this field are summarized.

关 键 词：三氟甲硫基化 三氟甲硒基化 三氟甲氧基化 三氟乙氧基化 ^18F-标记 

分 类 号：O621.25[理学—有机化学]