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

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.