Abstract:
In this work a new synthetic strategy aiming at the synthesis of [18F] labeled aromatic amino acids was developed and evaluated.
As model compounds, methoxy- and methyl- substituted benzenes, with one or two formyl-groups as activating auxiliary, were labeled by nucleophilic substitution with [18F]fluoride. The influence of different leaving groups (-F, -Cl, -Br, -NO2) and different reaction parameters on the radiochemical yield was examined. For the fast and efficient decarbonylation of these model compounds by Wilkinson’s Catalyst, the effect of temperature, reaction time and concentration was tested. The synthesis of 2-[18F]fluorotyrosine by the new synthetic concept for the labeling by [18F]fluoride in the presents of an (protected) amino acid residue was carried out successfully.