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Development of an automated system for synthesizing 18F-labeled compounds using [18F]fluoroethyl bromide as a
Ming-Rong Zhang1, Akio Tsuchiyama, Terushi Haradahira
1Department of Medical Imaging, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan.
Abstract:
An automated system was developed to synthesize 18F-labeled compounds using [18F]fluoroethyl bromide ([18F]FEtBr) as a synthetic precursor. The apparatus makes possible the following sequence of processes: (1) production of an aqueous solution of [18F]fluoride ([18F]F-), (2) recovery of [18F]F- from target chamber, (3) drying of [18F]F-, (4) formation and distillation of [18F]FEtBr into a trapping vessel, (5) alkylation of target compounds with [18F]FEtBr, (6) High performance liquid chromatography purification and (7) formulation. [18F]FEtBr, the synthetic precursor for fluoroethylation, was labeled via nucleophilic displacement of 2-trifluoromethanesulfonyloxy ethylbromide (BrCH2CH2OTf) with [18F]F- and was purified from the reaction mixture by distillation. After the conditions for forming [18F]FEtBr and drying [18F]F- were optimized, [18F]FEtBr was obtained in a radiochemical yield of 71 +/- 13% (n = 21, based on [18F]F-, corrected for decay) and a radiochemical purity of 98 +/- 1.4% at end of the syntheses (EOS). Using this automated system, [18F]fluoroethylspiperone ([18F]FEtSP) was prepared by reacting spiperone with [18F]FEtBr in a radiochemical yield and purity of 56 +/- 12% (n = 5, based on [18F]FEtBr, corrected for decay) and 97 +/- 1.5% with a specific activity of 310 +/- 120 GBq/mumol at EOS. The total synthesis time was 55 +/- 2.3 min from the end of bombardment and the developed system has proved to be reliable and reproducible.