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Technetium-99m labeled 2-nitroimidazole complex containing hydrazinyl nicotinamide group and preparation method and application of technetium-99m labeled 2-nitroimidazole complex

A kind of technology of nitroimidazoles and complexes, applied in the field of 2-nitroimidazoles complexes and preparation thereof

Active Publication Date: 2019-08-02
BEIJING NORMAL UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

There is currently no one 99m Tc-labeled tumor hypoxia imaging agents are popularized and applied in clinical practice, so a new type of drug that is convenient for clinical application has been developed. 99m Tc-labeled tumor hypoxia imaging agent has important practical significance

Method used

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  • Technetium-99m labeled 2-nitroimidazole complex containing hydrazinyl nicotinamide group and preparation method and application of technetium-99m labeled 2-nitroimidazole complex

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Embodiment Construction

[0048] The present invention is described in detail through the following examples: a technetium-99m-labeled 2-nitroimidazole complex containing hydrazino-nicotamide group, the general molecular formula expression of which is: 99m Tc(HYNICNM)(tricine / TPPTS), its structural formula is as follows:

[0049] ;

[0050] In the structural formula: the nitrogen atom on the hydrazine group in the HYNICNM molecule, the phosphorus atom in the co-ligand TPPTS, and the oxygen atom and nitrogen atom in the tricine and 99m Tc coordinates to get 99m Tc(HYNICNM)(tricine / TPPTS) complex, wherein n is an integer greater than and equal to 2.

[0051] 99m The preparation method of Tc (HYNICNM) (tricine / TPPTS) complex, its preparation steps are as follows:

[0052] a. Synthesis of ligand HYNICNM:

[0053] Weigh 0.440g of HYNIC hydrazone compound 1 containing NHS-activated ester and 0.156g of amino group-containing 2-nitroimidazole compound 2 into a 25mL round bottom flask, add 10mL DMF to ...

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Abstract

The invention discloses a 99mTc (HYNICNM) (tricine / TPPTS) complex and a preparation method and application thereof. The 99mTc (HYNICNM) (tricine / TPPTS) complex is obtained through two steps of synthesis of a ligand HYNICNM and preparation of a 99mTc (HYNICNM) (tricine / TPPTS) complex. The complex is simple and convenient to prepare and has oxygen deficiency selectivity. Tumor-bearing mice have highuptake and good retention in tumor parts, the tumor / non-target ratio is high, the uptake of non-target organs such as the liver and intestines is obviously reduced, and the 99mTc (HYNICNM) (tricine / TPPTS) complex is a novel tumor hypoxia imaging agent with excellent performance.

Description

technical field [0001] The invention belongs to the technical field of radiopharmaceuticals, and in particular relates to a technetium-99m-labeled hydrazino-nicotamide group-containing 2-nitroimidazole complex and a preparation method and application thereof. Background technique [0002] Tumors are a serious threat to human health. In recent years, there has been an increasing trend of younger age. Therefore, early diagnosis and treatment of tumors are of great significance to improve survival rate, prognosis and quality of life. In solid tumors, there are almost all hypoxic cells, and their ratio usually increases with the tumor volume. The higher the degree of tumor hypoxia, the greater the possibility of tumor malignancy, and the sensitivity to radiotherapy and certain chemotherapy drugs worse. Therefore, it is of great significance to detect tumor hypoxia to formulate treatment plan and improve treatment effect. There are several methods for detecting hypoxia, and rad...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F13/00C07B59/00A61K51/04A61P35/00A61K103/10
CPCA61K51/0478A61P35/00C07B59/00C07B2200/05C07F13/005
Inventor 张俊波阮晴甘倩倩张旭冉王学斌唐志刚陆洁张站斌
Owner BEIJING NORMAL UNIVERSITY
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