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Synthesis of a [18F]fluoroethyltriazolylthymidine radiotracer from [18F]2-fluoroethyl azide and 5-ethynyl-2′-deoxyuridine

✍ Scribed by U. Ackermann; G. O'Keefe; S.-T. Lee; A. Rigopoulos; G. Cartwright; J. I. Sachinidis; A. M. Scott; H. J. Tochon-Danguy

Publisher
John Wiley and Sons
Year
2011
Tongue
French
Weight
276 KB
Volume
54
Category
Article
ISSN
0022-2135

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✦ Synopsis

An improved synthesis for a fluoroethyltriazolylthymidine analog has been developed by employing the copper(I)catalyzed click chemistry reaction between 5-ethynyl-2 0 -deoxyuridine (EDU) and [ 19/18 F]2-fluoroethyl azide. When compared with the previously reported protocol the radiochemical yield has been increased from 3 to 32.572.5%. The synthesis time was 130 min and the specific activity ranged from 70.3 to 129.5 GBq/mmol. The tracer was found to be stable in human plasma and was subsequently evaluated in an A431 tumor model in BALB/c nude mice. Dynamic image acquisition using the Mosaic small animal PET scanner showed that the tumor to muscle ratio reached a maximum value of 2.1 from 22 min postinjection. These results indicate, that the fluoroethyltriazolylthymidine synthesized can be a promising radiotracer for tumor cell proliferation and thus become an important tool for treatment evaluation in oncology.

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