Journal Article

FZJ-2015-05017

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png A three-step radiosynthesis of 6-[ 18  F]fluoro- L-meta -tyrosine starting with [ 18  F]fluoride

Castillo Meleán, J. ; Ermert, J. (Corresponding author)FZJ* ; Coenen, H. H.FZJ*

2015
Wiley New York, NY [u.a.]

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Please use a persistent id in citations: doi:10.1002/jlcr.3273

Abstract: The radiosynthesis of 6-[18 F]fluoro-L-m-tyrosine has generally been performed by electrophilic radiofluorination, which exhibits several drawbacks. In the present work, a three-step radiochemical synthesis is described starting from [18 F]fluoride. The synthetic sequence, including isotopic exchange, Baeyer–Villiger oxidation, and hydrolysis, were examined comparing four fluorobenzophenone derivatives as labeling precursors. Of those, (2S,5S)-tert-butyl 5-(5-acetyl-2-fluorobenzyl)-2-tert-butyl-3-methyl-4-oxoimidazolidine-1-carboxylate (1a) and (2S,5S)-tert-butyl 2-tert-butyl-5-(2-fluoro-5-(2,2,2-trifluoroacetyl)benzyl)-3-methyl-4-oxoimidazolidine-1-carboxylate (1d) proved to be the most suitable ones. 6-[18 F]Fluoro-L-m-tyrosine was obtained with overall radiochemical yields of 8–13% and an enantiomeric excess of up to 98%.

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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 2015

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

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