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TcN(DGDTC)2 complexes as well as preparation method and use thereof

A technology of 99mtcn and complexes, applied in the fields of radiopharmaceutical chemistry and clinical nuclear medicine, can solve the problems of slow blood clearance, high blood background, and affecting imaging quality, etc.

Inactive Publication Date: 2009-05-06
BEIJING NORMAL UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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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  • TcN(DGDTC)2 complexes as well as preparation method and use thereof
  • TcN(DGDTC)2 complexes as well as preparation method and use thereof
  • TcN(DGDTC)2 complexes as well as preparation method and use thereof

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Embodiment Construction

[0043] Describe the present invention in detail below by embodiment:

[0044] A sort of 99m TcN (DGDTC) 2 Complexes:

[0045] a. Synthesis of ligand DGDTC:

[0046] 0.01mol glucosamine hydrochloride (analytically pure, produced by Alaf Aesar 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).

[0047] The theoretical value ω (%) of the mass fraction of each element is: C27.63, H4.93, N4.61, and the experimental value ω (%) is: C28.00, H5.20, N4.85.

[00...

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Abstract

The invention discloses a <99m> TcN(DGDTC)2 complex, a preparation method and application thereof. Taking the [<99m>Tc 3N] <2+> core as a central core, the complex has an irregular geometric configuration of square pyramid, wherein the N atom in the Tc3N triple bond is located at the acme, and the four sulphur atoms provided by two ligand CPFXDTC molecules are located at the four points on the bottom surface. The complex has the advantages of high radiochemical purity, good stability, simple preparation and low price, a higher uptake value and good residence in a tumor, and good target organ / non-target organ ratio such as tumor / blood ratio and tumor / muscle ratio. The complex is a novel tumor developer with high popularization and application value.

Description

Technical field [0001] The present invention relates to 99m The field of radiopharmaceutical chemistry and clinical nuclear medicine technology for TcN nuclear labeling, specifically relating to a 99m TcN(DGDTC)2 complex and its preparation method and application. Background technique [0002] At present, in the field of clinical medicine, malignant tumors have become the number one killer that endangers human health. In the treatment process of cancer patients, the most important factor is not the treatment method, but early diagnosis. Studies have shown that with early diagnosis and early treatment, 50% of tumor patients can be cured. At present, the methods used for early diagnosis of tumor mainly include: histological biopsy, X-ray method, magnetic resonance imaging (MRI) and radionuclide imaging and other methods. Radionuclide imaging can reflect changes in the physiology, pathology, metabolism, and function of tumors, and radionuclide imaging is a non-invasive dete...

Claims

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Application Information

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IPC IPC(8): C07F13/00C07H13/12A61K51/04A61K103/10
Inventor 张俊波任佳蕾王学斌唐志刚张现忠陆洁
Owner BEIJING NORMAL UNIVERSITY
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