硼酸
芳基
化学
组合化学
放射合成
有机化学
体内
烷基
生物技术
生物
作者
Chris Hoffmann,Niklas Kolks,Daniel Smets,Alexander Haseloer,Benedikt Gröner,Elizaveta A. Urusova,Heike Endepols,Felix Neumaier,Uwe Ruschewitz,Axel Klein,Bernd Neumaier,Boris D. Zlatopolskiy
标识
DOI:10.1002/chem.202202965
摘要
Cu-mediated radiofluorination is a versatile tool for the preparation of 18 F-labeled (hetero)aromatics. In this work, we systematically evaluated a series of complexes and identified several generally applicable mediators for highly efficient radiofluorination of aryl boronic and stannyl substrates. Utilization of these mediators in nBuOH/DMI or DMI significantly improved 18 F-labeling yields despite use of lower precursor amounts. Impressively, application of 2.5 μmol aryl boronic acids was sufficient to achieve 18 F-labeling yields of up to 75 %. The practicality of the novel mediators was demonstrated by efficient production of five PET-tracers and transfer of the method to an automated radiosynthesis module. In addition, (S)-3-[18 F]FPhe and 6-[18 F]FDOPA were prepared in activity yields of 23±1 % and 30±3 % using only 2.5 μmol of the corresponding boronic acid or trimethylstannyl precursor.
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