Chin. J. Org. Chem. ›› 2016, Vol. 36 ›› Issue (8): 1715-1740.DOI: 10.6023/cjoc201601009 Previous Articles     Next Articles

REVIEW

分子内直接引入含氟基团以及18F-标记方法研究进展

李恭铭, 孙德群   

  1. 山东大学(威海)海洋学院 威海 264209
  • 收稿日期:2016-01-09 修回日期:2016-02-16 发布日期:2016-04-15
  • 通讯作者: 孙德群 E-mail:dequn.sun@sdu.edu.cn

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

Li Gongming, Sun Dequn   

  1. Marine College, Shandong University at Weihai, Weihai 264209
  • Received:2016-01-09 Revised:2016-02-16 Published:2016-04-15

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, CF3O 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.

Key words: trifluoromethylthiolation, trifluoromethylselenolation, trifluoromethyloxylation, trifluoroethoxylation, 18F-labeling