Exploring Solvent Effects in the Radiosynthesis of ¹⁸F-Labeled Thymidine Analogues toward Clinical Translation for Positron Emission Tomography Imaging.

ABSTRACT: Thymidine analogues, 5-substituted 2'-deoxy-2'-[¹⁸F]fluoro-arabinofuranosyluracil derivatives, are promising positron emission tomography (PET) tracers being evaluated for noninvasive imaging of cancer cell proliferation and/or reporter gene expression. We report the radiosynthesis of 2'-deoxy-2'-[¹⁸F]fluoro-5-methyl-1-β-d-arabinofuranosyluracil ([¹⁸F]FMAU) and other 2'-deoxy-2'-[¹⁸F]fluoro-5-substituted-1-β-d-arabinofuranosyluracil analogues using 1,4-dioxane to replace the currently used 1,2-dichloroethane. Compared to 1,2-dichloroethane, 1,4-dioxane is analyzed as a better solvent in terms of radiochemical yield and toxicity concern. The use of a less toxic solvent allows for the translation of the improved approach to clinical production. The new radiolabeling method can be applied to an extensive range of uses for ¹⁸F-labeling of other nucleoside analogues.

SUBMITTER: Li J 

PROVIDER: S-EPMC7887844 | biostudies-literature | 2021 Feb

REPOSITORIES: biostudies-literature