常用^(18)F标记中间体的合成及其应用研究  

Studies on syntheses and applications of widely used ^(18)F-labeled intermediates

作　　者：王明伟[1] 尹端沚[1] 汪勇先[1] 

机构地区：[1]中国科学院上海应用物理研究所放射性药物研究中心,上海201800

出　　处：《核技术》2006年第1期63-71,共9页Nuclear Techniques

基　　金：国家自然科学基金(30371634);中国科学院知识创新工程重大项目(KJCX1-SW-08)资助

摘　　要：通过亲核放射氟化标记法,正电子核素[18F]氟被引入到目标分子中有两种途径:直接亲核放射氟化标记和间接亲核放射氟化标记。后者的关键是选择合适的标记中间体。本文根据18F–的取代位置,介绍了两大类、数十种标记中间体的合成及其在放射性药物合成领域中的应用。The positron-emitting nuclide fluorine-18 is of great importance to modem nuclear medicine with the increasing clinic demands of positron emission tomography （PET） and R＆D of PET radiopharmaceuticals worldwide. Fluorine-18 can be introduced into a target molecule to prepare the corresponding lSF-labeled radiopharmaceuticals through direct and indirect radiofluorinations. However, it is not suitable for the preparation of biomacromolecular-oriented radiopharmaceuticals such as peptides and protein using the direct labeling methods because of the lack of reaction selectivity. Thus, it is necessary to choose an appropriate ^18F-labeled intermediate for the indirect labeling methods. According to the classification of precursors displaced by lSF, this paper briefly introduces two species of ^18F-labeled intermediates originated from aliphatic and aromatic displacements and their syntheses and applications in PET radiopharmaceutical domain.

关 键 词：^18F 亲核放射氟化 标记中间体 

分 类 号：O621.3[理学—有机化学] O623[理学—化学]