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The present study reports a convenient method for   68 Ga-labelling under anhydrous conditions using solid-phase derived gallium-68-acetylacetonate ([  68 Ga]Ga(acac) 3 ) in a microwave-enhanced radiosynthesis. Commercial   68 Ge/ 68 Ga-radionuclide generators utilizing TiO 2  to adsorb   68 Ge(IV) (Obninsk-generators) were used. The initial aqueous generator eluate was transferred online onto a cation exchange resin and   68 Ga was absorbed quantitatively. From this resin,   68 Ga was eluted with different acetone-based, non-aqueous solvent systems. More than 95% of the generator-eluted   68 Ga was obtained from the cation exchange resin with 600 μL of a 98% acetone/2% acetylacetone mixture providing n.c.a. [  68 Ga]Ga(acac) 3  as labelling agent. Water-insoluble macrocyclic polypyrrole derivatives were chosen as model compounds for a proof-of-principle labelling of lipophilic compounds with   68 Ga. Labelling of two different porphyrin derivatives,   meso  -tetraphenyl-porphyrin (Tpp) and (3-(1-hydroxyheptyl)deuteroporphyrin dimethylester (HHDPD) was performed in chloroform in a focused microwave synthesis system in yields of up to 90% within 5 min using phenol as co-ligand. Moreover, new co-ligands were investigated to be more effective and significantly less toxic than phenol. Among the phenol alternatives, gentisic acid (2,5-dihydroxy benzoic acid, DHB, 5 mg) emerged as the most useful, non-toxic phenol substitute. It facilitates reducing the load of co-ligand by 95%, while providing an increased labeling yield of 97%.   68 Ga-labelled porphyrins may facilitate the medical application for molecular imaging   via   positron emission tomography.

Efficient post-processing of aqueous generator eluates facilitates 68 Ga-labelling under anhydrous conditions