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Click-to-Chelate: Development of Technetium and Rhenium-Tricarbonyl Labeled Radiopharmaceuticals

Division of Radiopharmaceutical Chemistry, Department of Radiology and Nuclear Medicine, University of Basel Hospital, Petersgraben 4, 4031 Basel
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Molecules 2013, 18(3), 3206-3226; https://doi.org/10.3390/molecules18033206
Received: 20 February 2013 / Revised: 5 March 2013 / Accepted: 6 March 2013 / Published: 12 March 2013
(This article belongs to the Collection Advances in Click Chemistry)
The Click-to-Chelate approach is a highly efficient strategy for the radiolabeling of molecules of medicinal interest with technetium and rhenium-tricarbonyl cores. Reaction of azide-functionalized molecules with alkyne prochelators by the Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC; click reaction) enables the simultaneous synthesis and conjugation of tridentate chelating systems for the stable complexation of the radiometals. In many cases, the functionalization of (bio)molecules with the ligand system and radiolabeling can be achieved by convenient one-pot procedures. Since its first report in 2006, Click-to-Chelate has been applied to the development of numerous novel radiotracers with promising potential for translation into the clinic. This review summarizes the use of the Click-to-Chelate approach in radiopharmaceutical sciences and provides a perspective for future applications. View Full-Text
Keywords: CuAAC; Click-to-Chelate; radiolabeling; radiopharmaceuticals; 99mTc-tricarbonyl; 186/188Re-tricarbonyl CuAAC; Click-to-Chelate; radiolabeling; radiopharmaceuticals; 99mTc-tricarbonyl; 186/188Re-tricarbonyl
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MDPI and ACS Style

Kluba, C.A.; Mindt, T.L. Click-to-Chelate: Development of Technetium and Rhenium-Tricarbonyl Labeled Radiopharmaceuticals. Molecules 2013, 18, 3206-3226.

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