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000202869 1001_ $$0P:(DE-HGF)0$$aCastillo Meleán, Johnny$$b0
000202869 245__ $$aA three-step radiosynthesis of 6-[ 18  F]fluoro- L-meta -tyrosine starting with [ 18  F]fluoride
000202869 260__ $$aNew York, NY [u.a.]$$bWiley$$c2015
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000202869 520__ $$aThe 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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000202869 7001_ $$0P:(DE-Juel1)131818$$aErmert, Johannes$$b1$$eCorresponding author$$ufzj
000202869 7001_ $$0P:(DE-Juel1)131816$$aCoenen, Heinrich Hubert$$b2$$ufzj
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