Synthesis of the first radiolabeled 188Re N-heterocyclic carbene complex and initial studies on its potential use in radiopharmaceutical applications

被引：10

作者：

Wagner, Thomas ^{[1
,2
]}

Zeglis, Brian M. ^{[3
]}

Groveman, Sam ^{[4
]}

Hille, Claudia ^{[1
,2
]}

Poethig, Alexander ^{[1
,2
]}

Francesconi, Lynn C. ^{[4
]}

Herrmann, Wolfgang A. ^{[1
,2
]}

Kuehn, Fritz E. ^{[1
,2
]}

Reiner, Thomas ^{[3
,5
]}

机构：

[1] Tech Univ Munich, Dept Chem, Chair Inorgan Chem Mol Catalysis, Garching, Germany

[2] Tech Univ Munich, Catalysis Res Ctr, Chair Inorgan Chem Mol Catalysis, Garching, Germany

[3] Mem Sloan Kettering Canc Ctr, Dept Radiol, Radiochem & Imaging Sci Serv, New York, NY 10021 USA

[4] CUNY Hunter Coll, New York, NY 10021 USA

[5] Mem Sloan Kettering Canc Ctr, Ctr Mol Imaging & Nanotechnol, New York, NY 10021 USA

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2014年 / 57卷 / 07期

关键词：

Re-188 carbene complex; radiopharmaceutical application; N-heterocyclic carbene; transmetalation; RADIATION SYNOVECTOMY AGENT; DIOXO COMPLEXES; THERAPEUTIC RADIOPHARMACEUTICALS; DIMERCAPTOSUCCINIC ACID; MONOCLONAL-ANTIBODIES; OLEFIN METATHESIS; BONE METASTASES; LIGANDS; RHENIUM; CANCER;

D O I：

10.1002/jlcr.3203

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

A novel approach towards the synthesis of radiolabeled organometallic rhenium complexes is presented. We successfully synthesized and analyzed the first Re-188-labeled N-heterocyclic biscarbene complex, trans-dioxobis(1,1'-methylene-bis(3,3'-diisopropylimidazolium- 2-ylidene)) (188)rhenium(V) hexafluorophosphate (Re-188-4) 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 for in vivo applications, the stability of the Re-188-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 new Re-188-labeled carbene complexes.

引用

页码：441 / 447

页数：7

共 45 条

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