Tejería María Emilia, Pereira María Pía, Gambini Juan Pablo, Duarte Pablo, Giglio Javier Gabriel, Rey Ana María
Área Radioquímica, Facultad de Química, Universidad de la República, Montevideo 11200, Uruguay.
Centro Uruguayo de Imagenología Molecular, CUDIM, Montevideo 11600, Uruguay.
Pharmaceuticals (Basel). 2024 Mar 18;17(3):388. doi: 10.3390/ph17030388.
"Click reactions" are a very useful tool for the selective conjugation of different molecular subunits to produce complex structures in a simple way. In this paper, we present the application of Cu(I)-catalyzed biorthogonal reactions between alkynes and azides to the indirect radiofluorination of an estradiol derivative with potential applications in estrogen receptor imaging. The procedure was fully developed on an automated synthesis platform, and conditions were optimized to achieve the desired product with a reasonable yield without precipitation. Although the biological results were not adequate for a potential radiopharmaceutical, the outcome of this work is valuable since the use of automated platforms is required for the reliable and reproducible preparation of PET radiopharmaceuticals in GMP conditions while limiting the radiation dose rates to the personnel.
“点击反应”是一种非常有用的工具，可用于不同分子亚基的选择性共轭，以简单的方式生成复杂结构。在本文中，我们展示了铜（I）催化的炔烃与叠氮化物之间的生物正交反应在雌二醇衍生物间接放射性氟化中的应用，该衍生物在雌激素受体成像中具有潜在应用。该方法在自动化合成平台上得到了充分发展，并对条件进行了优化，以合理产率获得所需产物且无沉淀。尽管生物学结果对于潜在的放射性药物而言并不充分，但这项工作的成果是有价值的，因为在药品生产质量管理规范（GMP）条件下可靠且可重复地制备正电子发射断层扫描（PET）放射性药物需要使用自动化平台，同时还要将人员所受辐射剂量率限制在一定范围内。
