AI Article Synopsis
- The study introduces a new three-step method for synthesizing 6-[(18)F]fluoro-L-m-tyrosine, addressing limitations of the traditional electrophilic radiofluorination method.
- The synthetic process involves isotopic exchange, Baeyer-Villiger oxidation, and hydrolysis, evaluated using four different fluorobenzophenone derivatives.
- The most effective precursors achieved overall radiochemical yields of 8-13% and an impressive enantiomeric excess of up to 98%.
Article 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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| http://dx.doi.org/10.1002/jlcr.3273 | DOI Listing |
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