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A Convenient Synthesis for HBED-CC-tris(tert-butyl ester)
Synlett ( IF 2 ) Pub Date : 2018-03-07 , DOI: 10.1055/s-0036-1591950
Ata Makarem 1 , Moritz Konrad 1 , Christos Liolios 1 , Klaus Kopka 1
Affiliation  

HBED-CC is a bifunctional complexing agent that, at ambient temperature, tightly chelates the trivalent radiometal 68 Ga (T 1/2 = 68 min). This complexing agent has attracted a lot of interest in tumor imaging applications. Depending on the chemical structure, different HBED-CC variants may be employed as radiolabeling precursor for the synthesis of desired radiopharmaceuticals. In this context, HBED-CC-tris(tert-butyl ester) is the only known monovalent variant of HBED-CC which is used for the synthesis of non-symmetric HBED-CC-based radiopharmaceuticals. Commercial HBED-CC-tris( tert -butyl ester) is very ­expensive, with limited availability. Nevertheless, no synthetic procedure for this useful product has been reported to date. This work introduces a convenient and comparatively cost-efficient method for the preparation of HBED-CC-tris( tert -butyl ester).

中文翻译:

HBED-CC-三(叔丁酯)的简便合成

HBED-CC 是一种双功能络合剂,可在环境温度下紧密螯合三价放射性金属 68 Ga(T 1/2 = 68 分钟)。这种络合剂引起了肿瘤成像应用的广泛兴趣。根据化学结构,不同的 HBED-CC 变体可用作合成所需放射性药物的放射性标记前体。在这种情况下,HBED-CC-三(叔丁酯)是 HBED-CC 唯一已知的单价变体,用于合成基于非对称 HBED-CC 的放射性药物。商用 HBED-CC-tris(叔丁酯)非常昂贵,供应有限。尽管如此,迄今为止还没有报道过这种有用产品的合成程序。
更新日期:2018-03-07
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