Synthesis of 4-([18F]fluoromethyl)-2-chlorophenylisothiocyanate: A novel bifunctional 18F-labelling agent
Gespeichert in:
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)
Online Zugang:
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| 024 | 7 | 0 | |a 10.1524/ract.92.4.349.35590 |2 doi |
| 035 | |a (NATIONALLICENCE)gruyter-10.1524/ract.92.4.349.35590 | ||
| 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 | |
| 700 | 1 | |a Wüst |D F. |4 aut | |
| 700 | 1 | |a Müller |D M. |4 aut | |
| 700 | 1 | |a Bergmann |D R. |4 aut | |
| 773 | 0 | |t Radiochimica Acta/International journal for chemical aspects of nuclear science and technology |d Oldenbourg Wissenschaftsverlag GmbH |g 92/4-6/2004(2004-04-01), 349-353 |x 0033-8230 |q 92:4-6/2004<349 |1 2004 |2 92 |o ract | |
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| 908 | |D 1 |a research article |2 jats | ||
| 950 | |B NATIONALLICENCE |P 856 |E 40 |u https://doi.org/10.1524/ract.92.4.349.35590 |q text/html |z Onlinezugriff via DOI | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Wüst |D F. |4 aut | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Müller |D M. |4 aut | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Bergmann |D R. |4 aut | ||
| 950 | |B NATIONALLICENCE |P 773 |E 0- |t Radiochimica Acta/International journal for chemical aspects of nuclear science and technology |d Oldenbourg Wissenschaftsverlag GmbH |g 92/4-6/2004(2004-04-01), 349-353 |x 0033-8230 |q 92:4-6/2004<349 |1 2004 |2 92 |o ract | ||
| 900 | 7 | |b CC0 |u http://creativecommons.org/publicdomain/zero/1.0 |2 nationallicence | |
| 898 | |a BK010053 |b XK010053 |c XK010000 | ||
| 949 | |B NATIONALLICENCE |F NATIONALLICENCE |b NL-gruyter | ||