Fast F-18 FDG synthesis by alkaline hydrolysis on a low polarity solid phase supports

in Journal of Labelled Compounds & Radiopharmaceuticals (2002), 45(5), 435-447

The synthesis of 2-deoxy-2-[18F]fluoro-D-glucose ([18F]FDG) has been simplified by the use of a tC18 Sep Pak cartridge to effect purification and hydrolysis of the tetraacetylated [18F]fluoro-glucose ... [more ▼]

The synthesis of 2-deoxy-2-[18F]fluoro-D-glucose ([18F]FDG) has been simplified by the use of a tC18 Sep Pak cartridge to effect purification and hydrolysis of the tetraacetylated [18F]fluoro-glucose compound ([18F]TAG). After radiolabelling, this derivative was trapped on a solid phase extraction (SPE) cartridge and the residual reaction solvent (CH3CN), reagents (K222, K2CO3,) and by-products removed by washing the support with water. After this cleaning step, the acetyl groups were cleaved on the same tC18 column using 2N sodium hydroxide. This fast reaction proceeded near quantitatively (>98%) at room temperature in less than 2 min. The [18F]FDG was then recovered with a small amount of water, neutralized with a slight excess of 2N hydrochloric acid, buffered for pH with a citrate solution and finally purified on a neutral alumina oxide and a second tC18 column. After filtration, the radiochemical yield of this [18F]FDG isotonic solution after more than 100 production runs was found to be very reliable and reproducible (70±6% decay corrected). The synthesis time was about 22 min. Quality controls showed that the radiochemical purity was higher than 98% and in any case no [18F]FDM was detected. Only traces of 2-chloro-2-deoxy-glucose (ClDG) were found in the final sample (64±9 g/ batch of 16 ml). [18F]FDG specific activity averaged between 1 and 20 Ci/µmol (EOS). No evaporation and use of ion retardation resin (AG11A8) are required. Moreover, this new approach is suitable for complete remote operation using available single use medical components. Copyright © 2002 John Wiley [less ▲]

In vivo studies of p-[18F]MPPF metabolites in human.

in Journal of Labelled Compounds & Radiopharmaceuticals (1999), 42

p-[18F]MPPF, a fluoro analog of WAY-100635 for visualisation of 5-HT1A receptors in cat.

in Journal of Labelled Compounds & Radiopharmaceuticals (1999), 42

Solid phase extraction : An alternative to the use of rotary evaporators for solvent removal in the rapid formulation of PET radiopharmaceuticals

in Journal of Labelled Compounds & Radiopharmaceuticals (1999), 42(1), 63-75

Solid phase extraction (SPE) was used for the formulation of several radiopharmaceuticals. The method involves dilution of the previously purified HPLC compound with water, trapping of the activity on an ... [more ▼]

Solid phase extraction (SPE) was used for the formulation of several radiopharmaceuticals. The method involves dilution of the previously purified HPLC compound with water, trapping of the activity on an SPE bed, washing off the support, elution of the radiopharmaceutical with a small volume of ethanol (<1 mL) and dilution with sterile isotonic saline solution. Recovery of the radiopharmaceuticals was always higher than 97%. Two different methods of automation were developed for the formulation of [11C] and [18F]radiopharmaceuticals. In all cases, organic solvent levels in the injectable solution were below the recommended limits. This fast (3-6 min.) and easy to automate process can be considered as an alternative to the conventional methods (rotary evaporators). Copyright © 1999 John Wiley [less ▲]

Metabolism of no carrier added 2-[18F]fluoro-L-tyrosine in free moving rats.

in Journal of Labelled Compounds & Radiopharmaceuticals (1997), 40

Synthesis of a fluorinated analogue of L-threo-3-(3,4-dihydroxyphenyl)serine: 6-fluoro-L-threo-DOPS.

in Journal of Labelled Compounds & Radiopharmaceuticals (1997), 40

Sep Pak as alternative to rotary evaporators for radiopharmaceutical formulations.

in Journal of Labelled Compounds & Radiopharmaceuticals (1995), 37

Fast quality control of short-lived radiopharmaceutical compounds with a photodiode array detector.

in Journal of Labelled Compounds & Radiopharmaceuticals (1995), 37

S-, N- and O-[11C]methylations of a Nor precursor adsorbed on Al2O3/KF.

in Journal of Labelled Compounds & Radiopharmaceuticals (1995), 37

11C-alkylation on Al2O3/MF: a useful method for rapid labelling.

in Journal of Labelled Compounds & Radiopharmaceuticals (1994), 35