King's College London, School of Biomedical Engineering and Imaging Sciences, Department of Imaging Chemistry and Biology, 4th Floor Lambeth Wing, St Thomas' Hospital, London, SE1 7EH, UK.
Chem Commun (Camb). 2021 May 18;57(40):4962-4965. doi: 10.1039/d1cc00495f.
Nitrogen-13 is an attractive but under-used PET radionuclide for labelling molecules of biological and pharmaceutical interest, complementing other PET radionuclides. Its short half-life (t1/2 = 9.97 min) imposes synthetic challenges, but we have expanded the hitherto limited pool of 13N labelling strategies and tracers by adapting the multicomponent Hantzsch condensation reaction to prepare a library of 13N-labelled 1,4-dihydropyridines from [13N]ammonia, including the widely-used drug nifedipine. This represents a key advance in 13N PET radiochemistry, and will serve to underpin the renewed interest in clinical opportunities offered by short-lived PET tracers.
氮-13 是一种有吸引力但未得到充分利用的正电子发射断层扫描（PET）放射性核素，可用于标记具有生物和药物学意义的分子，与其他 PET 放射性核素形成互补。其半衰期短（t1/2=9.97 分钟），这对合成提出了挑战，但我们通过改编多组分 Hantzsch 缩合反应，将迄今为止有限的 13N 标记策略和示踪剂库扩展到从[13N]氨中制备一系列 13N 标记的 1,4-二氢吡啶，包括广泛使用的药物硝苯地平。这是 13N PET 放射化学方面的一项重大进展，将为人们重新关注短寿命 PET 示踪剂带来的临床机会提供支持。
