D-glucose dithiocarbamate complex marked by TcO, preparation method and applications thereof

A kind of ammoniacalate, 99mtco technology, applied in the field of radiopharmaceutical chemistry and clinical nuclear medicine, can solve the problems of high blood background, slow blood clearance, affecting imaging quality and so on

Active Publication Date: 2009-10-14
BEIJING NORMAL UNIVERSITY +1
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Problems solved by technology

In the study, it was found that 99m Although Tc-labeled glucose derivatives have a high uptake in tumors, their blood clearance is slow and the blood background is high, which affects the imaging quality

Method used

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  • D-glucose dithiocarbamate complex marked by TcO, preparation method and applications thereof
  • D-glucose dithiocarbamate complex marked by TcO, preparation method and applications thereof
  • D-glucose dithiocarbamate complex marked by TcO, preparation method and applications thereof

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Embodiment

[0042] Describe the present invention in detail below by embodiment: a kind of 99m TcO(DGDTC) 2 Complexes:

[0043] a. Synthesis of ligand DGDTC:

[0044] 0.01mol glucosamine hydrochloride (analytically pure, produced by AlafAesar Company) was added to a 50mL three-necked flask, and 5mL of deionized water was added to dissolve it. , produced by Beijing Chemical Plant) aqueous solution, then slowly drop 0.01molCS 2 (analytical pure, Xilong Chemical Factory, Shantou City, Guangdong Province), stirred for 2h-3h, and the temperature during the entire reaction process was controlled below 10°C. The solvent was evaporated, and the residue was recrystallized from methanol to obtain a yellow powder, namely DGDTC. Its infrared spectrum data is: v(IR) / cm -1 : 3427(-OH), 2925(-CH 2 ), 1631(C-N), 1038(C=S).

[0045] The theoretical value ω (%) of the mass fraction of each element is: C 27.63, H 4.93, N 4.61, and the experimental value ω (%) is: C 28.00, H 5.20, N 4.85.

[0046] MS...

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Abstract

The invention discloses a D-glucose dithiocarbamate complex marked by TcO, a preparation method and applications thereof; the formula of the complex is TcO(DGDTC)2, takes Tc(V)O as a central nucleus and has a geometric configuration with the shape of an irregular square pyramid, wherein O atom in Tc=O bond is positioned at the top point and four sulphur atoms provided by two DGDTC ligand molecules are positioned at the four points of the bottom surface. By the technical steps of synthesis of ligand DGDTC and preparation of TcO (DGDTC)2 complex, the TcO (DGDTC)2 complex is obtained. The D-glucose dithiocarbamate complex has high radiochemical purity and good stability, has higher uptake value and good detention in tumor and higher ratio of tumor / muscle, and is suitable for being promoted and applied as a novel tumor imaging agent.

Description

Technical field [0001] The present invention relates to 99m The field of radiopharmaceutical chemistry and clinical nuclear medicine technology of TcO nuclear labeling, specifically relates to a 99m TcO core-labeled D-glucosaminolate complex, its preparation method and application. Background technique [0002] Today, malignant tumors have become the main killer of human health. In the prevention and treatment of tumors, the treatment method is not the most important, but the early diagnosis of tumors is the key. Studies have shown that with early diagnosis and early treatment, 50% of tumor patients can be cured. Radionuclide imaging can reflect changes in the physiology, pathology, metabolism, and function of tumors, and radionuclide imaging is a non-invasive detection method with many advantages that make radionuclide imaging the mainstay of tumor diagnosis. method. Among the many tumor imaging drugs, 18 F-fluorodeoxyglucose ([ 18 F]FDG) is currently the most widely...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H5/06C07H1/00C07F13/00A61K51/04A61K103/10
Inventor 张俊波任佳蕾林潇王学斌唐志刚张现忠陆洁
Owner BEIJING NORMAL UNIVERSITY
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