Labeling peptides, proteins and antibodies with fluorine-18 (18F-) has been performed using prosthetic groups such as N-succinimidyl-4-[18F]fluorobenzoate ([18F]SFB) and N-[6-(4-[18F]fluorobenzylidene)aminooxyhexyl]maleimide ([18F]FBAM).  However, these labeling methods often require multiple steps and results in low radiochemical yields.  Consequently, the search has been ongoing to develop a one step labeling prosthetic group.  A new class of chloropyrimidine compounds with different electron withdrawing/donating groups at the position meta to the chloro leaving group were investigated.  The 18F- radiolabeling was performed with the standard resolubilization method (drying the 18F- prior to labeling) and with the aqueous labeling conditions developed in our laboratory using the microfluidics.  Labeling was achieved and the radiochemical yields varied as a function of the functional group and labeling method.  The resultant [18F]fluoropyrimdines were stable up to 24 hrs.  This represents a promising single step labeling approach for new 18F- prosthetic groups.

Single step labeling approach to fluorine-18 prosthetic agents

243rd National Meeting (2012)

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