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The synthesis of [ 11 C]DASB is known to be performed by reacting the demethyl-DASB precursor with [ 11 C]methyl iodide but the necessary reaction parameters had hitherto not been determined. In this work the dependence of the labelling yield on reaction temperature, reaction time, precursor concentration and type of solvent was investigated. Best results were found when methylation was carried out at 100 °C within 2 min using 4 mg/ml demethyl precursor in DMSO. With respect to [ 11 C]methyl iodide a radiochemical yield of 74%±3% [ 11 C]DASB was achieved. In addition, the synthesis was transferred to a remotely controlled module. A carbon-11 production for 1 h at 50 μA resulted in 3800-4300 MBq [ 11 C]DASB with a specific activity of 152-211 GBq/μmol (4.1-5.7 Ci/μmol) (EOS) and a radiochemical purity of &gt;95% in a sterile solution ready for injection. The total synthesis time was 45 min after EOB.

radiochimica acta

Determination of reaction parameters for the synthesis of the serotonin transporter ligand [ 11 C]DASB: Application to a remotely controlled high yield synthesis