title: Maleimido-functionalized NOTA derivatives as bifunctional chelators for site-specific radiolabeling.
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.
authors.affiliation: Institute of Radiopharmacy, Helmholtz-Zentrum Dresden-Rossendorf, P.O. Box 510119, Dresden 01314, Germany. c.foerster@hzdr.de
authors.forename: Christian
authors.initials: C
authors.lastname: Förster
authors.forename: Maik
authors.initials: M
authors.lastname: Schubert
authors.forename: Hans-Jürgen
authors.initials: HJ
authors.lastname: Pietzsch
authors.forename: Jörg
authors.initials: J
authors.lastname: Steinbach
mesh_terms: D002614:Chelating Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000302:isolation & purification; D002851:Chromatography, High Pressure Liquid; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000302:isolation & purification; D006573:Heterocyclic Compounds, 1-Ring; D007553:Isotope Labeling; D008301:Maleimides / Q000138:chemical synthesis / Q000737:chemistry*; D055601:Organic Chemistry Phenomena
chemical_list: D002614:Chelating Agents; D006571:Heterocyclic Compounds; D006573:Heterocyclic Compounds, 1-Ring; D008301:Maleimides; C048993:1,4,7-triazacyclononane-N,N',N''-triacetic acid