Evaluation of two nucleophilic syntheses routes for the automated synthesis of 6-[F]fluoro-l-DOPA.

Two different strategies for the nucleophilic radiosynthesis of [F]F-DOPA were evaluated regarding their applicability for an automated routine production on an Ecker&Ziegler Modular-Lab Standard module. Initially, we evaluated a promising 5-step synthesis based on a chiral, cinchonidine-derived phase-transfer catalyst (cPTC) being described to give the product in high radiochemical yields (RCY), high specific activities (A) and high enantiomeric excesses (ee). However, the radiosynthesis of [F]F-DOPA based on this strategy showed to be highly complex, giving the intermediate products as well as the final product in insufficient yields for automatization.

Investigations into the synthesis, radiofluorination and conjugation of a new [¹⁸F]fluorocyclobutyl prosthetic group and its in vitro stability using a tyrosine model system.

The [(18)F]fluorocyclobutyl group has the potential to be a metabolically stable prosthetic group for PET tracers. The synthesis of the radiolabeling precursor cis-cyclobutane-1,3-diyl bis(toluene-4-sulfonate) 8 was obtained from epibromohydrin in 7 steps (2% overall yield). The radiolabeling of this precursor 8 and its conjugation to L-tyrosine as a model system was successfully achieved to give the new non-natural amino acid 3-[(18)F]fluorocyclobutyl-L-tyrosine (L-3-[(18)F]FCBT) [(18)F]17 in 8% decay-corrected yield from the non-carrier-added [(18)F]fluoride.

5-(2-18F-fluoroethoxy)-L-tryptophan as a substrate of system L transport for tumor imaging by PET.

Unlabelled: Large neutral l-amino acids are substrates of system L amino acid transporters. The level of one of these, LAT1, is increased in many tumors. Aromatic l-amino acids may also be substrates of aromatic l-amino acid decarboxylase (AADC), the level of which is enhanced in endocrine tumors.

Faster analysis of radiopharmaceuticals using ultra performance liquid chromatography (UPLC) in combination with low volume radio flow cell.

With the aim of reducing analysis time of radiopharmaceuticals, especially for carbon-11 and fluorine-18, radio-high performance liquid chromatography (radio-HPLC) is the analysis method of choice. Faster and more sensitive analytic methods are needed. Recently, ultra performance liquid chromatography (UPLC) has become an accepted analysis method but has not yet been established in radiopharmacy.

Strategy for improved [(11)C]DAA1106 radiosynthesis and in vivo peripheral benzodiazepine receptor imaging using microPET, evaluation of [(11)C]DAA1106.

Introduction: The peripheral benzodiazepine receptor (PBR) has shown considerable potential as a clinical marker of neuroinflammation and tumour progression. [(11)C]DAA1106 ([(11)C]N-(2,5-dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)-acetamide) is a promising positron emission tomography (PET) radioligand for imaging PBRs.

Methods: A four-step synthetic route was devised to prepare DAA1123, the precursor for [(11)C]DAA1106.