Method for preparation of fluorine-18-labeled flumazenil using diaryliodonium salt precursor
AssigneeBio Imaging Korea Co., Ltd.
InventorsByung Chul Lee, Byung Seok Moon, Ji Sun Kim
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Abstract
Disclosed is the synthesis of [18F]flumazenil that is useful in imaging epileptic lesions by PET (positron emission tomography). A method for preparing [18F]flumazenil by reacting a diaryliodonium salt precursor with the positron-emitting radionuclide fluorine-18. [18F]flumazenil can be prepared from the diaryliodonium salt precursor in the presence of kryptofix2.2.2./potassium carbonate(K2.2.2./K2CO3) and TEMPO in dimethylformamide (DMF) at a high yield.
Claims3
A method for preparing fluorine-18-labeled flumazenil, comprising reacting a diaryliodonium salt precursor with fluorine-18 at 130 to 160° C. in the presence of a phase transition catalyst which is selected from the group consisting of kryptofix2.2.2./potassium carbonate (K2.2.2./K2CO3), tetrabutylammonium hydroxide (TBAOH), tetrabutylammonium bicarbonate (TBAHCO3), cesium hydroxide (CsOH), and a combination thereof,
- wherein the diaryliodonium salt precursor is represented by the following Chemical Formula 1:
- wherein Ar− is selected from the group consisting of the following aryl (Ar−) radicals:
- and X− is selected from among trifluoromethane sulfonate), perfluoro C2-C10 alkyl sulphonate, trifluoroacetate, tetraphenylborate), toluene sulfonate), Br−, and Cl−.
A method for preparing fluorine-18-labeled flumazenil, comprising reacting a diaryliodonium salt precursor with fluorine-18, wherein the diaryliodonium salt precursor is represented by the following Chemical Formula 2:
- wherein —Ar is
- R1˜R3 independently selected from among H, C1 alkyl, C2 alkyl, C1 haloalkyl, and C2 haloalkyl, and X− is selected from among trifluoromethane sulfonate, perfluoro C2-C10 alkyl sulphonate, trifluoroacetate, tetraphenylborate, toluene sulfonate, Br−, and Cl−.
Dependencies are inferred from the claim text.