[18F]fluoro-β-fluoromethylene-m-tyrosine analogs, potential PET agents for presynaptic dopamine terminals: Synthesis and spectroscopic characterization
✍ Scribed by Dhanabalan Murali; Onofre T. DeJesus; John J. Sunderland; R.Jerome Nickles
- Book ID
- 103922937
- Publisher
- Elsevier Science
- Year
- 1992
- Weight
- 823 KB
- Volume
- 43
- Category
- Article
- ISSN
- 0883-2889
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✦ Synopsis
18F-labeled (E)-beta-fluoromethylene-DL-m-tyrosine (FMMT) was prepared by the direct reaction of FMMT with [18F]acetylhypofluorite (AcOF) resulting into three product isomers. Extensive 1H, 13C and 19F-NMR spectroscopic analysis identify these products to be 2-fluoro, 6-fluoro-FMMT and 2,6-difluoro-FMMT. The HPLC isolated radiochemical EOB yields of these products were 22, 25 and 14%, respectively, based on starting [18F]AcOF. The specific activity at the end of a synthesis time of an hour was ca 200 mCi/mmol. With the possible advantage of "metabolic trapping" in dopamine nerve terminals via covalent binding to MAO and reduced metabolite formation, [18F]F-FMMT may potentially be the optimal PET tracer for CNS dopamine nerve terminals.