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Molecules 2011, 16(6), 5228-5240; doi:10.3390/molecules16065228
Article

Maleimido-Functionalized NOTA Derivatives as Bifunctional Chelators for Site-Specific Radiolabeling

* , ,  and
Institute of Radiopharmacy, Helmholtz-Zentrum Dresden-Rossendorf, P.O. Box 510119, Dresden 01314, Germany
* Author to whom correspondence should be addressed.
Received: 24 May 2011 / Revised: 10 June 2011 / Accepted: 17 June 2011 / Published: 22 June 2011
(This article belongs to the Section Organic Synthesis)
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Abstract

Two basic and simple synthetic routes for mono- and bis-maleimide bearing 1,4,7-triazacyclononane-N,N’,N’’-triacetic acid (NOTA) chelators as new bifunctional chelators are described. The syntheses are characterized by their simplicity and short reaction times, as well as practical purification methods and acceptable to very good chemical yields. The usefulness of these two synthetic pathways is demonstrated by the preparation of a set of mono- and bis-maleimide functionalized NOTA derivatives. In conclusion, these two methods can easily be expanded to the syntheses of further tailored maleimide-NOTA chelators for diverse applications.
Keywords: 1,4,7-triazacyclonone-1,4,7-triacetic acid; NOTA; site-specific; maleimide; ethylene glycol spacer 1,4,7-triazacyclonone-1,4,7-triacetic acid; NOTA; site-specific; maleimide; ethylene glycol spacer
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Förster, C.; Schubert, M.; Pietzsch, H.-J.; Steinbach, J. Maleimido-Functionalized NOTA Derivatives as Bifunctional Chelators for Site-Specific Radiolabeling. Molecules 2011, 16, 5228-5240.

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