Microwave improved synthesis of p-[18F]MPPF, 5-HT1A antagonist and PET sudies on cat brain.

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

Synthesis of [18F]FDG with alkaline hydrolysis on a low polarity solid phase support.

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

Tissue distribution, autoradiography and metabolism in rats of p-[18F]MPPF: 5-HT1A antagonist.

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

Evaluation of p-[18F]MPPF, 5-HT1A antagonist, a potential radiopharmaceutical for PET: tissue distribution, autoradiography and metabolism in rats.

in Society for Neuroscience / Abstracts (1997), 23

No-carrier-added asymmetric synthesis of alpha-methyl-alpha-amino acids labelled with fluorine-18

in Tetrahedron (1997), 53(16), 5785-5796

Various [18F]fluoro aromatic α-methyl-L-amino acids 11 have been synthesized with high enantiomeric purity (ee > 97%). These new radiopharmaceuticals for Positron Emission Tomography (PET), potential ... [more ▼]

Various [18F]fluoro aromatic α-methyl-L-amino acids 11 have been synthesized with high enantiomeric purity (ee > 97%). These new radiopharmaceuticals for Positron Emission Tomography (PET), potential inhibitors of enzymatic functions, were regiospecifically labelled by nucleophilic substitution on trimethylammoniumbenzaldehyde triflate precursors 9. The [18F]fluoro aromatic aldehydes 12 obtained were easily converted to the corresponding [18F]fluorobenzyl halides [13 (X = 1)]. After alkylation of the lithium enolate of (2S,5S)-l-tert-Boc-2-tert-butyl-3,5-dimethyl-imidazolidin-4-one 2, the adducts were cleaved to give, after HPLC purification, various [18F]fluoro-α-methyl amino acid analogs with radiochemical yields of 10% (End of Bombardment, EOB) after a synthesis time of 120 min. The corresponding [19F]fluorinated amino acids 4 and [19F]fluoro intermediates were also prepared. [less ▲]

Enantioselective syntheses of no-carrier-added (nca) (S)-4-chloro-2 F-18 fluorophenylalanine and (S)-(alpha-methyl)-4-chloro-2 F-18 fluorophenylalanine

in Journal of Fluorine Chemistry (1996), 80(2), 117-124

(S)-4-Chloro-2-fluorophenylalanine and (S)-( a-methyl)-4-chloro-2-fluorophenylalanine were synthesized and labeled with no carrier added (n.c.a.) fluorine-18 through a radiochemical synthesis relying on ... [more ▼]

(S)-4-Chloro-2-fluorophenylalanine and (S)-( a-methyl)-4-chloro-2-fluorophenylalanine were synthesized and labeled with no carrier added (n.c.a.) fluorine-18 through a radiochemical synthesis relying on the highly enantioselective reaction between 4-chloro-2-[18F] fluorobenzyl iodide and the lithium enolate of (2s) -1-( tert-butyloxycarbonyl) -2-( tert-butyl)-3-methyl- 1,3-imidazolidine-4-one for (S) -4-chloro-2- [18F] fluorophenylalanine and (2S,5S)-1-( tert-butyloxycarbonyl) -2-( tert-butyl) -3,5-dimethyl- 1,3-imidazolidine-4-one for (S) -( a-methyl) -4-chloro-2- [18F] fluorophenylalanine. Quantities of about 20-25 mCi were obtained at the end of synthesis, ready for injection after hydrolysis and high performance liquid chromatography (HPLC) purification, with a radiochemical yield of 17%-20% corrected to the end of bombardment after a total synthesis time of 90-105 min from [18F] fluoride. The enantiomeric excesses were shown to be 97% or more for both molecules without chiral separation and the radiochemical and chemical purities were 98% or better. [less ▲]

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

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

Sep Pak as alternative to rotary evaporators for radiopharmaceutical formulations.

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

Fast Routine Production of L-[11C-methyl]methionine with Al2O3KF

in Applied Radiation & Isotopes (1995), 46(9), 893-897

No-carrier-added (nca) L-[11C-methyl]methionine was prepared via the very fast S-alkylation of L-homocysteine adsorbed on AI203/KF with [11C]iodomethane at room temperature in ethanol. The alkylation was ... [more ▼]

No-carrier-added (nca) L-[11C-methyl]methionine was prepared via the very fast S-alkylation of L-homocysteine adsorbed on AI203/KF with [11C]iodomethane at room temperature in ethanol. The alkylation was realized with a radiochemical yield of 94 +/- 4% EOB (n = 20). More than 90% (n = 20) of the precursor L-homocysteine remained adsorbed on the solid support and was eliminated by a simple filtration. After reaction, neither racemization nor by-product were detected. The purification process was thus limited to a C18 Sep-Pak followed by an alumina Sep-Pak. The radiochemical purity measured on the final solution was shown to be > 99%. The only chemical contaminant was L-homocysteine (+ 10 µg). With this new technique, L-[11C-methyl]methionine was ready for injection within 10 min from [11C]CO2 with a specific activity ranging around 37 + 5.6 GBq (1 +/- 0.15 Ci)//tmol EOB. Through this procedure L-[11C-methyl]methionine can be prepared without preparative HPLC purification, This is an important simplification for the fast routine production of one of the most widely used radiopharmaceutical compounds for PET. [less ▲]