Bio Imaging Korea Co., Ltd.

Snu Rdb Foundation

Byung Seok Moon

Byung Chul Lee

Ji Sun Kim

Sang Eun Kim

Jae Ho Jung

Yu Kyeong Kim

The present invention relates to tricarbonyl technetium-99m or rhenium-188 labeled cyclic RGD derivatives, a preparation method thereof, and a pharmaceutical composition containing the derivative as an active ingredient for use in the diagnosis or treatment (radiotherapy) of angiogenesis-related diseases. The tricarbonyl technetium-99m or rhenium-188 labeled cyclic RGD derivatives of the present invention has a high subnanomolar affinity to integrin &#x3b1;&#x3b2;(also called as a vitronectin receptor) that is activated in an angiogenic action induced by a tumor, and acts exclusively upon cancer cells having selectively activated integrin &#x3b1;&#x3b2;because of a substantially low intake into the liver and intestines.

Tricarbonyl technetium-99m, rhenium-185/187, or rhenium-188 labeled cyclic RGD derivatives and uses thereof

Disclosed is the synthesis of [F]flumazenil that is useful in imaging epileptic lesions by PET (positron emission tomography). A method for preparing [F]flumazenil by reacting a diaryliodonium salt precursor with the positron-emitting radionuclide fluorine-18. [F]flumazenil can be prepared from the diaryliodonium salt precursor in the presence of kryptofix/potassium carbonate(K/KCO) and TEMPO in dimethylformamide (DMF) at a high yield.

Method for preparation of fluorine-18-labeled flumazenil using diaryliodonium salt precursor

A method for preparing [F]fallypride is disclosed, which comprises a first step for trapping a fluorine-18 to a polymer ion exchange cartridge; a second step for extraction of fluorine-18 by inputting low base concentrations: 5.0&#x2dc;25 &#x3bc;L of 40% TBAHCOor K2.2.2./KCO(5&#x2dc;25 mg/0.5&#x2dc;3.0 mg) as a phase-transfer catalyst in a mixture of alcohol/water (1.0/0.2 (v/v)) or alcohol as a solvent into the polymer ion exchange cartridge trapped by the fluorine-18; a third step for preparing a [F]fallypride product by removing the solvent from the trapped fluorine-18, by inputting tosylate precursor in CHCN as a solvent into a reactor and by reacting the same for 5&#x2dc;35 minutes at 50&#x2dc;120&#xb0; C.; and a fourth step for preparing a pure [F]fallypride by purifying the prepared [F]fallypride product.

Growing community of inventors

Seoul, South Korea

Byung Seok Moon