biostudies-literatureUnknown13(2)Yang H<b>Rationale:</b> Conventional ¹⁸F-labeling methods that demand substrate pre-modification or lengthy radiosynthesis procedures have impeded the visualization and translation of numerous biomolecules, as biomarkers or ligands, using modern positron emission tomography techniques <i>in vivo</i>. Moreover, ¹⁸F-labeled biomolecules in high molar activity (A_m) that are indispensable for sensitive imaging could be only achieved under strict labeling conditions. <b>Methods:</b> Herein, ¹⁸F-labeled fluorothiophosphate (FTP) synthons in high A_m have been generated rapidly <i>in situ</i> in reaction solutions with < 5% water <i>via</i> nucleophilic substitution by wet [¹⁸F]F^-, which required minimal processing from cyclotrTheranostics472-482https://www.ebi.ac.uk/biostudies/studies/S-EPMC9830440biostudies-literatureSimplified one-pot ¹⁸F-labeling of biomolecules with <i>in situ</i> generated fluorothiophosphate synthons in high molar activity.PMC9830440Yang HLiu HHe FLi JLi ZZhang YZhang LChen XMou ZfalseSimplified one-pot ¹⁸F-labeling of biomolecules with <i>in situ</i> generated fluorothiophosphate synthons in high molar activity.<b>Rationale:</b> Conventional ¹⁸F-labeling methods that demand substrate pre-modification or lengthy radiosynthesis procedures have impeded the visualization and translation of numerous biomolecules, as biomarkers or ligands, using modern positron emission tomography techniques <i>in vivo</i>. Moreover, ¹⁸F-labeled biomolecules in high molar activity (A_m) that are indispensable for sensitive imaging could be only achieved under strict labeling conditions. <b>Methods:</b> Herein, ¹⁸F-labeled fluorothiophosphate (FTP) synthons in high A_m have been generated rapidly <i>in situ</i> in reaction solutions with < 5% water <i>via</i> nucleophilic substitution by wet [¹⁸F]F^-, which required minimal processing from cyclotr2023-01-01T00:00:00Z20232025-04-04T21:55:05.198Z2025-02-18T23:36:59.988ZS-EPMC98304403663222610.7150/thno.79452