Recent Trends in the Nucleophilic [18F]-radiolabeling Method with No-carrier-added [18F]fluoride

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In vivo biodistribution of no-carrier-added 6-18F-fluoro-3,4-dihydroxy-L-phenylalanine (18F-DOPA), produced by a new nucleophilic substitution approach, compared with carrier-added 18F-DOPA, prepared by conventional electrophilic substitution.

UNLABELLED A novel synthetic approach to 6-(18)F-fluoro-3,4-dihydroxy-L-phenylalanine ((18)F-DOPA), involving the nucleophilic substitution of a diaryliodonium salt precursor with non-carrier-added (18)F-fluoride, yielded a product with a specific activity that was 3 orders of magnitude higher than the product of the conventional synthesis method, involving an electrophilic substitution of a tr...

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Recovery and purification of no-carrier-added [18F]fluoride with bistrimethylsilylsulfate (BTMSS).

No-carrier-added trimethylsilyl[18F]fluoride (TMS[18F]F) was rapidly liberated from a variety of dry supports containing unreactive [18F]fluoride by simply heating with neat bistrimethylsilylsulfate. The supports included calcium phosphate, anion exchange resins, alumina, borosilicate and porous carbon beads, to which [18F]fluoride was applied by absorption or evaporation of aqueous solution. T...

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Production at the Curie level of no-carrier-added 6-18F-fluoro-L-dopa.

UNLABELLED 6-(18)F-fluoro-L-dopa ((18)F-FDOPA) has proven to be a useful radiopharmaceutical for the evaluation of presynaptic dopaminergic function using PET. In comparison to electrophilic synthesis, the no-carrier-added (NCA) nucleophilic method has several advantages. These include much higher available activity and specific activity. Recently, we have described an NCA enantioselective synt...

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

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Oxidation of substituted 4-fluorobenzaldehydes: application to the no-carrier-added syntheses of 4-[18F]fluoroguaiacol and 4-[18F]fluorocatechol.

The synthesis of 4-[18F]fluoroguaiacol (4-[18F]fluoro-2-methoxyphenol) has been achieved in no-carrier-added form starting from 2-methoxy-4-nitrobenzaldehyde, using nucleophilic aromatic substitution by [18F]fluoride followed by Baeyer-Villiger oxidation of the benzaldehyde to the phenol. Demethylation with boron tribromide gave 4-[18F]fluorocatechol (1,2-dihydroxy-4-[18F]fluorobenzene) with an...

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ژورنال

عنوان ژورنال: Nuclear Medicine and Molecular Imaging

سال: 2010

ISSN: 1869-3474,1869-3482

DOI: 10.1007/s13139-009-0008-1