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99mtc marked glucose derivative and preparation method and application thereof

A technology of 99mtc and 99mtc-cbadg, applied in the field of glucosamine derivatives and their preparation, can solve the problems of slow blood clearance, affecting imaging quality, and low target/non-target ratio.

Inactive Publication Date: 2013-03-27
BEIJING NORMAL UNIVERSITY
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Problems solved by technology

99m Tc-ECDG blood clearance is slow and the target / non-target ratio is low, which affects the imaging quality

Method used

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  • 99mtc marked glucose derivative and preparation method and application thereof
  • 99mtc marked glucose derivative and preparation method and application thereof
  • 99mtc marked glucose derivative and preparation method and application thereof

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Embodiment Construction

[0043] Describe the present invention in detail below by embodiment: a class 99m The Tc-labeled glucosamine derivative is to convert amino-D-glucose into 2-(4-carboxy-1-butyramide)-2-deoxy-D-glucose ligand (CBADG), and then carry out its 99m Tc direct labeling and 99m Tc(CO) 3 Nuclear markers were prepared into corresponding 99m Tc-CBADG and 99m Tc(CO) 3 -CBADG complexes.

[0044] 99m The preparation method of the glucosamine derivative (CBADG) of Tc mark is as follows:

[0045] a. Synthesis of ligand CBADG:

[0046] Add 1g of glucosamine hydrochloride (analytically pure, produced by AlafAesar) into a 25mL round bottom flask, add 2mL of deionized water to dissolve, then add 0.68mL of triethylamine, cool the resulting solution with an ice-water bath, and add 5mL of 0.116g / mL acetone / glutaric anhydride (analytical grade, produced by Beijing Chemical Plant) solution was stirred for 4 hours, and the temperature during the entire reaction process was controlled below 0°C to...

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Abstract

The invention provides a tumoraffin 99mTc marked glucosamine derivative (CBADG) and a preparation method and an application thereof. The preparation method comprises the following steps: converting amino-D-glucose into 2-(4-carboxyl-1-butylamide)-2-deoxy-D-glucose ligand (CBADG), and then marking directly with 99mTc and 99mTc(CO)3 to obtain the corresponding complex of 99mTc-CBADG and 99mTc(CO)3-CBADG. The complex of 99mTc-CBADG and 99mTc(CO)3-CBADG prepared by the invention has the advantages of high radiochemical purity, high ratio of tumor / blood and tumor / muscle, and is favorable for tumor intake and detention and the like, and the novel tumor image agent prepared by the complex is worthy to be popularized.

Description

technical field [0001] The present invention relates to 99m Tc-labeled radiopharmaceutical chemistry and clinical nuclear medicine technology, specifically related to 99m Tc-labeled glucosamine derivative (CBADG) and its preparation method and application. Background technique [0002] Tumor is a new organism formed when a certain cell in a local tissue loses normal regulation of its growth at the gene level under the action of various carcinogenic factors, resulting in its clonal abnormal proliferation. It is a serious hazard to human health. Disease is also one of the hot spots of scientific research. At present, malignant tumors have become the main killer of human health. According to the Beijing Municipal Health Bureau, the top five causes of death in Beijing are malignant tumors, cerebrovascular diseases, heart disease, respiratory diseases, and injury and poisoning. Among them, tumors accounted for 24.55% of the total deaths. In the process of tumor treatment, the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H5/06C07H1/00A61K51/04A61K103/10
Inventor 张俊波王跃朱菁菁陆洁王学斌唐志刚
Owner BEIJING NORMAL UNIVERSITY
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