Abstract
The study describes the development of a simple and effective method for 18F-fluoroethylation -omitting the azeotropic drying step- by elution of a [18F]fluoride loaded QMA column with a K2CO3/K222/acetonitrile solution containing 2–3% (v/v) water directly to the 1,2-ethylene glycol-bis-tosylate precursor. In acetonitrile containing 2–3% (v/v) water the labeling agent 2-[18F]fluoroethyl tosylate ([18F]FETs) was formed in 76–96% non-isolated radiochemical yield. The method was exemplified on the 18F-fluoroethylation of three COX-2 inhibitors with different core structures. The superiority of the so called “hydrous 18F-fluoroethylation” is characterized by a minimum loss of [18F]fluoride, by fivefold increased radiochemical yield of isolated final radiotracers and by shortened overall reaction time, in comparison to conventional approach.
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