Ligand-Enabled Copper-Mediated Radioiodination of Arenes
Ligand-Enabled Copper-Mediated Radioiodination of Arenes
复制标题
DOI：
10.1021/acs.orglett.4c00356
复制
发表时间：
2024-02-09
期刊：
影响因子：
5.2
通讯作者：
Sutherland，Andrew
中科院分区：
文献类型：
--
作者：
McErlain，Holly;Andrews，Matthew J.;Sutherland，Andrew
铜预催化剂的发现，促进芳烃卤代脱硼的关键机械步骤，使含放射性碘的芳烃的合成步骤的变化。活性预催化剂[Cu（0Ac）（phen）2] 0Ac被示出以1- 2mol%的负载量和10 min的反应时间进行芳基硼酸的室温放射性碘脱硼。这些温和的条件能够实现特别清洁的反应，如放射性药物和SPECT示踪剂间碘苄胍（MIBG）的有效制备所证明的。
The discovery of a copper precatalyst that facilitates the key mechanistic steps of arene halodeboronation has allowed a step change in the synthesis of radioiodine-containing arenes. The active precatalyst [Cu(OAc)(phen)2]OAc was shown to perform room temperature radio-iododeboronation of aryl boronic acids with 1–2 mol % loadings and 10 min reaction times. These mild conditions enable particularly clean reactions, as demonstrated with the efficient preparation of the radiopharmaceutical and SPECT tracer,meta-iodobenzylguanidine (MIBG).