Bloux Hugo, Dahiya Amit, Hébert Alexandra, Fabis Frédéric, Schoenebeck Franziska, Cailly Thomas
Centre d'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Normandie Univ, UNICAEN, 14000, Caen, France.
Institute of Organic Chemistry, RWTH Aachen University, Landoltweg 1, 52074, Aachen, Germany.
Chemistry. 2023 Apr 3;29(19):e202203366. doi: 10.1002/chem.202203366. Epub 2023 Mar 1.
The radio-iodination of arenes is investigated from organosilane and organogermane precursors using ipso-electrophilic halogenation (IEH). Discovery of a mild base mediated process allows radio-iodination in HFIP (1,1,1,3,3,3-hexafluoro-2-propanol) of either aryl silane or germane, with germanes being more reactive. Clinical potential of arylgermanes as radio-iodination precursors is demonstrated through the labelling of [ I]IMTO (iodometomidate) and [ I]MIBG (meta-iodobenzylguanidine) thus offering an alternative to radio-iododestannylation processes using non-toxic precursors.
利用本位亲电卤化反应（IEH），从有机硅烷和有机锗烷前体出发，对芳烃的放射性碘化反应进行了研究。发现了一种温和碱介导的过程，该过程可实现芳基硅烷或锗烷在HFIP（1,1,1,3,3,3-六氟-2-丙醇）中的放射性碘化反应，其中锗烷的反应活性更高。通过对[I]IMTO（碘代美托咪酯）和[I]MIBG（间碘苄胍）进行标记，证明了芳基锗烷作为放射性碘化前体的临床潜力，从而为使用无毒前体的放射性脱锡反应提供了一种替代方法。
