Journal Article

FZJ-2016-07110

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Efficient synthesis of [$^{18}$ F]FPyME: A new approach for the preparation of maleimide-containing prosthetic groups for the conjugation with thiols

Cavani, M. ; Bier, D. (Corresponding author)FZJ* ; Holschbach, M.FZJ* ; Coenen, H. H.FZJ*

2017
Wiley New York, NY [u.a.]

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Please use a persistent id in citations: doi:10.1002/jlcr.3469

Abstract: An improved high yielding radiosynthesis of the known thiol-reactive maleimide-containing prosthetic group1-[3-(2-[18F]fluoropyridine-3-yloxy)propyl]pyrrole-2,5-dione ([18F]FPyME) is described. The target compound was obtained by a two-step one-pot procedure starting from a maleimide-containing nitro-precursor that was protected as a Diels-Alder adduct with 2,5-dimethylfurane. Nucleophilic radiofluorination followed by heat induced deprotection through a Retro Diels Alder reaction yielded, after chromatographic isolation, [18F]FPyME with a radiochemical yield of 20% in about 60 min overall synthesis time. A variety of other [18F]fluoropyridine based maleimide-containing prosthetic groups should be accessible via the described synthetic strategy.

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Contributing Institute(s):

1. Nuklearchemie (INM-5)

Research Program(s):

1. 573 - Neuroimaging (POF3-573) (POF3-573)

Appears in the scientific report 2017

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Database coverage:
; BIOSIS Previews ; Current Contents - Life Sciences ; Current Contents - Physical, Chemical and Earth Sciences ; IF < 5 ; JCR ; Nationallizenz ; SCOPUS ; Science Citation Index ; Science Citation Index Expanded ; Thomson Reuters Master Journal List ; Web of Science Core Collection

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