Synthesis of 4-[18F]fluoro-L-m-tyrosine: a model analog for the in vivo assessment of central dopaminergic function

Int J Rad Appl Instrum A. 1990;41(9):801-7. doi: 10.1016/0883-2889(90)90056-m.

Abstract

4-[18F]Fluoro-L-m-tyrosine (6), a new analog of L-dopa for probing the presynaptic dopaminergic system by positron emission tomography has been synthesized in good radiochemical yields via the regioselective fluorodemercuration of the 4-mercurio derivatives 4a and 4b with 18F-labeled acetylhypofluorite. The chemical, radiochemical and enantiomeric purities were determined to be greater than 99%. The key step in the synthesis of the precursors 4 was the mercuration of the protected L-m-tyrosine 3. The position of mercuration on the aromatic ring was gleaned from the 13C-NMR spectral data. The non-radiolabeled counterpart of 6 was also synthesized. Structural analyses of all these compounds were carried out by 1H-, 13C-, 19F-NMR and mass spectroscopy.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Fluorine Radioisotopes*
  • Magnetic Resonance Spectroscopy
  • Tomography, Emission-Computed*
  • Tyrosine / analogs & derivatives*
  • Tyrosine / chemical synthesis
  • Tyrosine / chemistry

Substances

  • Fluorine Radioisotopes
  • 4-fluoro-3-tyrosine
  • Tyrosine