Synthesis of the first radiolabeled 188Re N-heterocyclic carbene complex and initial studies on its potential use in radiopharmaceutical applications.
Synthesis of the first radiolabeled 188Re N-heterocyclic carbene complex and initial studies on its potential use in radiopharmaceutical applications.
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第一个放射性标记 188Re N-杂环卡宾配合物的合成及其在放射性药物应用中的潜在用途的初步研究。
DOI：
10.1002/jlcr.3203
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发表时间：
2014
影响因子：
1.8
通讯作者：
Reiner,Thomas
中科院分区：
文献类型：
--
作者：
Wagner,Thomas;Zeglis,BrianM;Groveman,Sam;Hille,Claudia;Pöthig,Alexander;Francesconi,LynnC;Herrmann,WolfgangA;Kühn,FritzE;Reiner,Thomas
提出了一种合成放射性标记金属有机稀土配合物的新方法。我们成功地合成了第一个188Re标记的N-杂环双卡宾配合物trans‐dioxobis(1，1′‐methylene‐bis(3，3′‐diisopropylimidazolium‐2‐ylidene))188rhenium(V)六氟磷酸盐(188Re-4)，它是一个空气稳定、湿度稳定的银(I)双卡宾配合物。为了评估该配合物作为潜在的铅结构在活体应用中的可行性，在生理相关的介质中测试了188Re-NHC配合物的稳定性。最终，我们的研究表明，我们合成的络合物解离速度很快，因此不适合用于放射性药物。然而，很明显，我们开发的转金属化方法是一种快速、可靠和温和的方法来合成新的188Re标记的卡宾配合物。版权所有©2014 John Wiley&Sons，Ltd.
A novel approach towards the synthesis of radiolabeled organometallic rhenium complexes is presented. We successfully synthesized and analyzed the first188Re‐labeledN‐heterocyclic biscarbene complex,trans‐dioxobis(1,1′‐methylene‐bis(3,3′‐diisopropylimidazolium‐2‐ylidene))188rhenium(V) hexafluorophosphate (188Re‐4) via transmetalation using an air‐stable and moisture‐stable silver(I) biscarbene complex. In order to assess the viability of this complex as a potential lead structure forin vivoapplications, the stability of the188Re‐NHC complex was tested in physiologically relevant media. Ultimately, our studies illustrate that the complex we synthesized dissociates rapidly and is therefore unsuitable for use in radiopharmaceuticals. However, it is clear that the transmetalation approach we have developed is a rapid, robust, and mild method for the synthesis of new188Re‐labeled carbene complexes. Copyright © 2014 John Wiley & Sons, Ltd.