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3′[ 18 F]Fluoro-3′-deoxy-thymidine ([ 18 F]FLT) (III) has been discussed to be a promising tracer for assessing tumor proliferation. In order to perform clinical studies for evaluating [ 18 F]FLT a simplified labeling procedure was developed using 2,3′-anhydrothymidine with benzoyl as a protecting group in the 5′-position (I). In DMSO the labeling yield was 46% at 160 °C in 10 min. Hydrolysis was efficiently performed with 0.25% NaOH at room temperature within 10 min. The labeling procedure was transferred to a remote controlled synthesis module allowing the production of [ 18 F]FLT in high activities. The overall radiochemical yield was 18.1 ± 5.4% ( n  = 55) with absolute yields of 9.2 ± 2.6 GBq of [ 18 F]FLT at EOS ready for injection (60 min after EOB; irradiation parameters: 35 μA, 60 min) and specific activities of 100–220 GBq/μmol. A convenient cartridge method for metabolite analysis was developed and validated  versus  HPLC showing that after 90 min 69.0 ± 7.0% of the radioactivity in plasma (less than 20% of initial radioactivity) was unchanged [ 18 F]FLT (26 patients with various tumors).

Simplified, automated synthesis of 3′[ 18 F]fluoro-3′-deoxy-thymidine ([ 18 F]FLT) and simple method for metabolite analysis in plasma