Department of Radiology, Memorial Sloan Kettering Cancer Center, New York, New York, USA.
Department of Radiology, Weill Cornell Medical College, New York, New York, USA.
J Labelled Comp Radiopharm. 2020 Jul;63(9):419-425. doi: 10.1002/jlcr.3847. Epub 2020 Jun 16.
In this paper, we disclose a new strategy for the radiosynthesis of [ F]PARPi from the corresponding, boc-protected, nitro-precursor. Using a two-step procedure, [ F]PARPi could be isolated in radiochemical yields up to 9.6%. The reaction proceeds via an efficient one-pot, two-step process, allowing for simplification over previous methods that require complex multi-step, multi-pot strategies to be implemented.
在本文中,我们披露了一种从相应的 Boc 保护的硝基前体来放射性合成 [ F]PARPi 的新策略。采用两步法,[ F]PARPi 的放射性化学收率最高可达 9.6%。该反应通过高效的一锅两步法进行,简化了以前需要采用复杂的多步、多釜策略的方法。