Author/Authors :
Oliver Roehn، نويسنده , , Ulrike and Becaud، نويسنده , , Jessica and Mu، نويسنده , , Linjing and Srinivasan، نويسنده , , Ananth and Stellfeld، نويسنده , , Timo and Fitzner، نويسنده , , Ansgar and Graham، نويسنده , , Keith and Dinkelborg، نويسنده , , Ludger and Schubiger، نويسنده , , August P. and Ametamey، نويسنده , , Simon M.، نويسنده ,
Abstract :
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.
Keywords :
PET , Nucleophilic ring-opening , aziridine , Biomolecule , Fluorine-18
