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<99m>tc marked dimercapto succinate metronidazole esters complex and preparation method and use

A technology of metronidazole dimercaptosuccinate and 99mtc, which is applied in the fields of radiopharmaceutical chemistry and clinical nuclear medicine, and can solve the problems that the growth rate of blood vessels cannot meet the growth of tumors, insufficient blood supply, and hypoxia of tumors

Inactive Publication Date: 2011-09-07
BEIJING NORMAL UNIVERSITY +1
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Problems solved by technology

In solid tumors, most tumors grow quite rapidly, and the growth rate of blood vessels cannot meet the growth of the tumor, resulting in a serious shortage of blood supply, resulting in hypoxia in the tumor

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  • &lt;99m&gt;tc marked dimercapto succinate metronidazole esters complex and preparation method and use
  • &lt;99m&gt;tc marked dimercapto succinate metronidazole esters complex and preparation method and use
  • &lt;99m&gt;tc marked dimercapto succinate metronidazole esters complex and preparation method and use

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Embodiment Construction

[0039] Describe the present invention in detail below by embodiment:

[0040] A sort of 99m Tc-labeled metronidazole dimercaptosuccinate complexes:

[0041] (1) Synthesis of ligand DMSAme:

[0042] Suspend 360mg of dimercaptosuccinic acid (DMSA) and 1.10g of metronidazole in 15mL of anhydrous pyridine, and add 500mg of N,N'-dicyclohexylcarbodiimide (DCC) dropwise in an ice-water bath pyridine solution, reacted at room temperature for 24 hours after dropping, evaporated pyridine to dryness under reduced pressure to obtain a black oil, dissolved the residue in 20mL dichloromethane (CH 2 Cl 2 ), the insoluble matter was filtered off, and the solution was successively washed with 5% NaHCO 3 , saturated NaCl solution and water, and the organic phase was washed with anhydrous NaCl 2 SO 4 After drying, spin dry CH under reduced pressure 2 Cl 2 , a yellow solid was obtained with a yield of 29%. DMSAme infrared spectrum data:

[0043] IR(KBr) / cm -1 : 2852(-SH), 1708(C=O), 15...

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Abstract

The present invention discloses a <99m> Tc labeled metronidazolyl dimercaptosuccinate complex (DMSAme) and a preparation method thereof. The complex takes [<99m>Tc]<3+> as a centronucleus and has an irregular square pyramid-shaped geometric configuration, wherein an oxygen atom of a Tc=O bond is at a top vertex, and four sulphur atoms of two DMSAme ligand molecules are at four vertexes of a bottom surface. The complex has high radiochemical purity, good stability, good uptake value and retention in tumors and high tumor to muscle ratio, can be widely used in imaging of tumors in human and animal organs, and is a novel tumor hypoxia imaging agent with high promotion and use value.

Description

Technical field [0001] The present invention relates to 99m Tc-labeled radiopharmaceutical chemistry and clinical nuclear medicine technology, especially related to a 99m Tc-labeled metronidazole dimercaptosuccinate complex, preparation method and application. Background technique [0002] In recent years, malignant tumors, usually called cancer, have become the most serious disease that endangers human health and seriously affect human health. Therefore, the research on tumor imaging drugs is one of the hot spots in radiopharmaceutical research today. In terms of imaging, due to 99m Tc has excellent nuclear properties such as short half-life (6.02 hours) and moderate gamma-ray energy (140 keV), making it suitable for in vivo imaging in conjunction with SPECT (Single-Photo Emission Computed Tomography) , and the radiation dose to the patient is very low. medical 99 Mo- 99m The successful research of Tc generator makes 99m Tc nuclide is easy to obtain and cheap, so 99...

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F13/00C07D233/91A61K51/04A61K103/10
Inventor 张俊波于倩杨胜何艺宁唐亭婷杨琛琛王学斌唐志刚张现忠陆洁
Owner BEIJING NORMAL UNIVERSITY
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