Syntheses of High‐Valent fac‐[99mTcO3]+ Complexes and [3+2] Cycloadditions with Alkenes in Water as a Direct Labelling Strategy |
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Authors: | Henrik Braband Dr Yuji Tooyama Thomas Fox Dr Roger Alberto Prof Dr |
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Institution: | Institute of Inorganic Chemistry, University of Zürich, Winterthurerstrasse 190, 8057 Zürich (Switzerland), Fax: (+41)?44?635?68?03 |
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Abstract: | Reported herein is a new concept for the labelling of biomolecules with small 99 mTcO3]+ complexes through a 3+2] cycloaddition with alkenes for radiopharmaceutical applications. We developed convenient reactions for the synthesis of small, water stable fac‐TcO3(tacn‐R)]+ complexes (99Tc and 99mTc, tacn=1,4,7‐triazacyclononane, R=H, ‐CH2‐C6H5, ‐CH2‐C6H4COOH). With alkenes, these high valent 99mTcO3]+ complexes undergo 3+2] cycloaddition with formation of the corresponding TcV–glycolato complexes. The 99mTcV and 99mTcVII complexes are stable at 37 °C in water and in the presence of serum proteins. Therefore, new opportunities in technetium chemistry are enabled with a high potential for medicinal and biological applications. In contrast to classical labelling, the presented strategy is ligand and not metal‐centred. |
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Keywords: | alkenes cycloaddition labelling medicinal chemistry radiopharmacy technetium |
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