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Abstract
[18F]-N-succinimidyl 4-(fluoromethyl)benzoate (1) has been prepared from N-succinimidyl-4-[(4-nitrobenzensulfonyl)oxymethyl]benzoate
(2) in one step using Kryptofix 2.2.2/[18F-]. The effect of solvents, potassium salts
and temperatures were studied to determine optimum labeling condition. The best results
were obtained using carbonate as the counter ion and acetone as the solvent at room
temperature. Overall radiochemical yields of approximately 18% (EOS) for the synthesis
of 1 were obtained in 30-35 min, including HPLC purification. Proteins were labeled
with 1 with labeling yields of 50-70% in 15 min.