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Caobonyl technetium labeled 2-azomycin composition, preparation method and application

A technology of nitroimidazole and carbonyl technetium, applied in the field of radionuclide-labeled compounds, can solve the problems of no substantial breakthrough in clinical imaging value, unsatisfactory clinical imaging performance, slow tissue clearance, etc., and achieve good imaging diagnosis. Results, good tumor hypoxic cell affinity, effect of improving drug uptake

Inactive Publication Date: 2010-02-24
LANZHOU UNIVERSITY
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  • Abstract
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  • Claims
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Problems solved by technology

[0004] Tumor hypoxia imaging agents that have been used in clinical research include 18 FMISO, 99m Tc-HL91, 64 Cu-ATSM, etc., but their clinical imaging performance is not ideal. The main problems include low absolute tumor uptake, slow clearance of normal tissues, radioactive concentration in the liver and abdomen, etc.
In order to obtain tumor hypoxia imaging agents with better imaging properties, researchers at home and abroad have conducted extensive and in-depth research and explored a series of 18 F. 99m Tc, 123 / 125 I and 62 / 64 Cu and other labeled nitroimidazole or non-nitroimidazole derivatives, but unfortunately there is no substantial breakthrough in clinical imaging value of these derivatives

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  • Caobonyl technetium labeled 2-azomycin composition, preparation method and application
  • Caobonyl technetium labeled 2-azomycin composition, preparation method and application
  • Caobonyl technetium labeled 2-azomycin composition, preparation method and application

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Embodiment Construction

[0040] A specific example of the present invention is given below, in which the degree of polymerization n of the polyethylene glycol linking group used is 3.

[0041] Synthesis of Pegylated 2-Nitroimidazole Ligand

[0042] Compound 1a (Tetraethylene glycol di(p-toluenesulfonate)): Dissolve tetraethylene glycol (5.82g, 30mmol) and triethylamine (9.1g, 90mmol) in 30mL of dichloromethane, slowly add p-toluenesulfonyl chloride dropwise (12.6g, 66mmol) dissolved in dichloromethane (30mL) solution, after the reaction at room temperature was continued for 4 hours, the solid was removed by suction filtration, the filtrate was washed 4 times, the organic phase was dried and the solvent was removed in vacuo to obtain 12.67g of viscous liquid (25.2 mmol, 84%). 1 H NMR (400MHz, CDCl 3 ): δ=2.45(s, 6H, OCH 3 ), 3.57(s, 8H), 3.68(t, 4H, J=4.5Hz), 4.15(t, 4H, J=4.5Hz), 7.34(d, 4H, J=8.1Hz), 7.79(d, 4H , J=8.1Hz), ppm.

[0043] Compound 2a (2-(2-(2-(2-(2-nitro-1H-imidazol-1-yl)ethoxy)et...

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Abstract

The invention discloses a radioactive nuclide labeled compound which is caobonyl technetium labeled 2-azomycin composition, a preparation method of the compound and a purpose of the compound. The preparation method of the caobonyl technetium labeled 2-azomycin composition comprises the following steps: firstly synthesizing a ligand NC-PEGn-NIM and heating the ligand and a newly prepared midbody <99m>Tc(CO)3(H2O)3<+>, the pH value of which is regulated to 9 to 10, to obtain the caobonyl technetium labeled 2-azomycin composition. The caobonyl technetium labeled 2-azomycin composition is concentrated in anoxybiotic tumor cells by the targeting function of azomycin and can be used for the SPECT raster display diagnosis of anoxybiotic tumors.

Description

technical field [0001] The present invention relates to a class of compounds labeled with radioactive nuclides, as well as the preparation method and application of the compounds. Specifically, the present invention relates to carbonyl technetium-labeled 2-nitroimidazole complexes. Background technique [0002] Malignant tumor is one of the main diseases that lead to abnormal death of human beings, and it ranks in the forefront of disease mortality and cause of death in my country and the world. Hypoxia is a common characteristic of human and animal tumors. Experimental observation and measurement show that the proportion of hypoxic cells in solid tumors is generally 10-20%, and some even reach 50%. At present, the treatment methods for malignant tumors are mainly radiotherapy and chemotherapy in addition to surgery, but hypoxia makes tumor tissue insensitive to radiotherapy and chemotherapy, which greatly improves its resistance to radiotherapy and chemotherapy; at the same...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F13/00C07D233/91A61K51/04A61K103/10
Inventor 汪建军谈存敏牛婷婷吴王锁
Owner LANZHOU UNIVERSITY
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