Universität zu Köln

Zlatopolskiy, Boris D., Zischler, Johannes ORCID: 0000-0003-3996-7473, Urusova, Elizaveta A., Endepols, Heike ORCID: 0000-0002-6166-4818, Kordys, Elena, Frauendorf, Holm, Mottaghy, Felix M. and Neumaier, Bernd ORCID: 0000-0001-5425-3116 (2015). A Practical One-Pot Synthesis of Positron Emission Tomography (PET) Tracers via Nickel-Mediated Radiofluorination. ChemistryOpen, 4 (4). S. 457 - 463. WEINHEIM: WILEY-V C H VERLAG GMBH. ISSN 2191-1363

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Abstract

Recently a novel method for the preparation of F-18-labeled arenes via oxidative [F-18] fluorination of easily accessible and sufficiently stable nickel complexes with [F-18] fluoride under exceptionally mild reaction conditions was published. The suitability of this procedure for the routine preparation of clinically relevant positron emission tomography (PET) tracers, 6[-F-18]fluorodopamine (6-[F-18]FDA), 6-[F-18]fluoro-l-DOPA (6-[F-18]FDOPA) and 6-[F-18]fluoro-m-tyrosine (6-[F-18]FMT), was evaluated. The originally published base-free method was inoperative. However, a low base protocol afforded protected radiolabeled intermediates in radiochemical conversions (RCCs) of 5-18 %. The subsequent deprotection step proceeded almost quantitatively (> 95 %). The simple one-pot two-step procedure allowed the preparation of clinical doses of 6-[F-18]FDA and 6-[F-18]FDOPA within 50 min (12 and 7% radiochemical yield, respectively). In an unilateral rat model of Parkinson's disease, 6-[F-18]FDOPA with high specific activity (175 GBq mu mol(-1)) prepared using the described nickel-mediated radiofluorination was compared to 6-[F-18] FDOPA with low specific activity (30 MBq mu mol(-1)) produced via conventional electrophilic radiofluorination. Unexpectedly both tracer variants displayed very similar in vivo properties with respect to signal-to-noise ratio and brain distribution, and consequently, the quality of the obtained PET images was almost identical.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Zlatopolskiy, Boris D. UNSPECIFIED UNSPECIFIED UNSPECIFIED Zischler, Johannes UNSPECIFIED orcid.org/0000-0003-3996-7473 UNSPECIFIED Urusova, Elizaveta A. UNSPECIFIED UNSPECIFIED UNSPECIFIED Endepols, Heike UNSPECIFIED orcid.org/0000-0002-6166-4818 UNSPECIFIED Kordys, Elena UNSPECIFIED UNSPECIFIED UNSPECIFIED Frauendorf, Holm UNSPECIFIED UNSPECIFIED UNSPECIFIED Mottaghy, Felix M. UNSPECIFIED UNSPECIFIED UNSPECIFIED Neumaier, Bernd UNSPECIFIED orcid.org/0000-0001-5425-3116 UNSPECIFIED
URN:	urn:nbn:de:hbz:38-396849
DOI:	10.1002/open.201500056
Journal or Publication Title:	ChemistryOpen
Volume:	4
Number:	4
Page Range:	S. 457 - 463
Date:	2015
Publisher:	WILEY-V C H VERLAG GMBH
Place of Publication:	WEINHEIM
ISSN:	2191-1363
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language FLUORINATION; METABOLISM; DIAGNOSIS; SYSTEM Multiple languages Chemistry, Multidisciplinary Multiple languages
URI:	http://kups.ub.uni-koeln.de/id/eprint/39684