Solid-phase supported direct F-radiofluorination of peptides.
作者信息
Fernandes Eduardo F A, Knudsen Line B S, Kjaer Andreas, Strømgaard Kristian, Herth Matthias M
机构信息
Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2 DK-2100 Copenhagen, Denmark.
Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2 DK-2100 Copenhagen, Denmark; Department of Clinical Physiology, Nuclear Medicine & PET and Cluster for Molecular Imaging, Copenhagen University Hospital - Rigshospitalet, Blegdamsvej 9 DK-2100 Copenhagen, Denmark; Department of Biomedical Sciences, University of Copenhagen Blegdamsvej 3 DK-2200 Copenhagen, Denmark.
出版信息
Bioorg Med Chem Lett. 2025 May 1;120:130118. doi: 10.1016/j.bmcl.2025.130118. Epub 2025 Jan 30.
The absence of universal and expedient labeling procedures hampers the widespread application of peptides as molecular tracers for positron emission tomography (PET). In this work, we have developed a proof-of-concept direct radiofluorination procedure for peptides using conventional solid-phase peptide synthesis. The method is compatible with all standard amino acids and enables the generation of a range of peptide-based radiopharmaceuticals archieving radiochemical yields of up to 30 % and radiochemical purities above 95 %.
Zotero 插件