有机催化剂辅助的Ar-F键形成：直接芳香族放射性氟化的通用方法。
Organocatalyst-assisted Ar-F bond formation: a universal procedure for direct aromatic radiofluorination.
作者信息
Jakobsson Jimmy Erik, Grønnevik Gaute, Riss Patrick Johannes
机构信息
Realomics Strategic Research Initiative, Department of Chemistry, Faculty for Mathematics and Natural Sciences, University of Oslo, Norway.
出版信息
Chem Commun (Camb). 2017 Nov 30;53(96):12906-12909. doi: 10.1039/c7cc07211b.
A metal free, phosphane-catalysed protocol for C-F bond formation based on ipso-elimination of iodanes is described. The reaction proceeds in significantly higher yield and with markedly reduced variability of yields (yield range) than previously described procedures. Rapid and efficient radiofluorination is achieved using unobjectionable chemical reagents with precedence in routine radiotracer production. With operational ease and mild conditions, the method promises a high potential for radiolabelling of biomolecules.
描述了一种基于碘烷的原位消除的无金属、膦催化的碳-氟键形成方法。与先前描述的方法相比，该反应的产率显著更高，产率的变异性（产率范围）明显降低。使用在常规放射性示踪剂生产中具有先例的无问题化学试剂可实现快速有效的放射性氟化。该方法操作简便、条件温和，有望在生物分子放射性标记方面具有很高的潜力。
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