کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1315244 | 976014 | 2009 | 11 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Nucleophilic ring-opening of activated aziridines: A one-step method for labeling biomolecules with fluorine-18 Nucleophilic ring-opening of activated aziridines: A one-step method for labeling biomolecules with fluorine-18](/preview/png/1315244.png)
The direct labeling of biomolecules with fluorine-18 is highly desirable. An option is the ring-opening of an activated aziridine moiety in a biomolecule using 18F-fluoride. Therefore, a series of aziridine-based model compounds and three aziridine-based biomolecules four aziridine-based model compounds were synthesized and evaluated as potential precursors for a direct one-step radiolabeling with fluorine-18. High to moderate yields of 18F-incorporation were achieved under mild labeling conditions. The influence of different activating groups, reaction temperature, solvent and base was investigated. The applicability of this method for the direct 18F-radiolabeling of biomolecules for positron emission tomography (PET) studies is illustrated with examples.
A one-step radiolabeling of model compounds and biomolecules with fluorine-18 has been achieved via nucleophilic ring-opening of activated aziridines (see Scheme). High to moderate yields of 18F-incorporation were achieved under mild labeling conditions. One-step 18F-labeling of model compounds and biomolecules via nucleophilic ring-opening of activated aziridines.Figure optionsDownload as PowerPoint slide
Journal: Journal of Fluorine Chemistry - Volume 130, Issue 10, October 2009, Pages 902–912