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US 10,869,942 B2Granted
Method
AssigneeNorsk Medisinsk Syklotronsenter AS
InventorsDag Erlend Olberg, Anders Svadberg
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Abstract
The present invention relates to new and improved methods of synthesizing radiolabelling agents which can be used to label biomolecules for use as radiopharmaceuticals. It further relates to certain novel radiolabelling agents and their use in such methods. PET imaging methods and methods of diagnosis employing such radiolabelling agents form a further aspect of the invention.
Claims16
A radiofluorination process comprising:
- (a) providing a solid stationary phase which comprises a polymeric anion-exchange resin having bound thereto [18F]fluoride anions;
- and
- (b) contacting said solid stationary phase with a non-aqueous solution comprising a precursor compound of formula (I):
- and a solvent selected from acetonitrile, tent-butanol, dimethylformamide, dimethylsulphoxide, dimethylacetamide, tetrahydrofuran, dioxan, 1,2-dimethoxyethane, sulpholane, N-methylpyrolidinone, or mixtures thereof, or an ionic liquid, optionally in the presence of an organic non-nucleophilic base,
- whereby to produce a radiofluorinated compound of formula (II):
- wherein:
- in formula (I), L is a positively charged leaving group;
- and in formulae (I) and (II), R is a group of the formula:
- wherein R′ is an electron-withdrawing group,
- wherein the radiofluorination process is performed at a temperature of from 10° C. to 25° C., and wherein the stationary phase is not contacted with a phase transfer catalyst during step (b).
7 more elements
Dependencies are inferred from the claim text.