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Synthesis of a [ 18 F]fluoroethyltriazolylthymidine radiotracer from [ 18 F]2‐fluoroethyl azide and 5‐ethynyl‐2′‐deoxyuridine
Author(s) -
Ackermann U.,
O'Keefe G.,
Lee S.T.,
Rigopoulos A.,
Cartwright G.,
Sachinidis J. I.,
Scott A. M.,
TochonDanguy H. J.
Publication year - 2011
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1863
Subject(s) - chemistry , azide , click chemistry , deoxyuridine , radiochemistry , specific activity , pet imaging , yield (engineering) , chemical synthesis , nuclear chemistry , nuclear medicine , combinatorial chemistry , positron emission tomography , biochemistry , in vitro , organic chemistry , medicine , dna , materials science , metallurgy , enzyme
An improved synthesis for a fluoroethyltriazolylthymidine analog has been developed by employing the copper(I)‐catalyzed click chemistry reaction between 5‐ethynyl‐2′‐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 32.5 ± 2.5%. The synthesis time was 130 min and the specific activity ranged from 70.3 to 129.5 GBq/µmol. 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. Copyright © 2011 John Wiley & Sons, Ltd.