Synthesis of 4-([18F]fluoromethyl)-2-chlorophenylisothiocyanate: A novel bifunctional 18F-labelling agent

Verfasser / Beitragende:
[F. Wüst, M. Müller, R. Bergmann]
Ort, Verlag, Jahr:
2004
Enthalten in:
Radiochimica Acta/International journal for chemical aspects of nuclear science and technology, 92/4-6/2004(2004-04-01), 349-353
Format:
Artikel (online)
ID: 378907301
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024 7 0 |a 10.1524/ract.92.4.349.35590  |2 doi 
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245 0 0 |a Synthesis of 4-([18F]fluoromethyl)-2-chlorophenylisothiocyanate: A novel bifunctional 18F-labelling agent  |h [Elektronische Daten]  |c [F. Wüst, M. Müller, R. Bergmann] 
520 3 |a The one-step radiosynthesis of 4-([18F]fluoromethyl)-2-chlorophenylisothiocyanate 18F-7 as a novel bifunctional 18F-labelling agent is described. Optimised reaction conditions in a remotely controlled synthesis module gave isothiocyanate 18F-7 in radiochemical yields of 45% (decay-corrected) within 40min and high radiochemical purity of >95% after solid-phase-extraction. Coupling of compound 18F-7 with the primary amine benzylamine as a model reaction afforded the corresponding ((4-[18F]fluoromethyl)-2-chloro-phenyl)-benzyl thiourea 18F-8 in a high radiochemical yield of >90%. Stability studies of thiourea 18F-8 in terms of radiodefluorination showed appreciable buffer stability at pH 7.4, whereas significant radiodefluorination was observed when 18F-8 was incubated in buffers at pH 3.6 and pH 9.4. Preliminary dynamic PET studies with thiourea 18F-8 in male Wistar rats showed high bone accumulation, indicative of high in vivo radiodefluorination. 
540 |a © 2004 Oldenbourg Wissenschaftsverlag GmbH 
690 7 |a Laboratory techniques, experiments  |2 nationallicence 
690 7 |a Analytical chemistry  |2 nationallicence 
690 7 |a Inorganic chemistry  |2 nationallicence 
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700 1 |a Müller  |D M.  |4 aut 
700 1 |a Bergmann  |D R.  |4 aut 
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