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Ligand compound for image diagnosis and its preparing method and compound for image diagnosis and its intermediate preparation

A technology of compounds and ligands, applied in the field of ligand compounds used for imaging diagnosis and preparation and imaging diagnosis compounds and intermediates for preparation thereof

Inactive Publication Date: 2008-04-23
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

but due to 99m The distribution of Tc-ECDG showed tumor / blood and tumor / lung ratios less than 1.0, lower than 18 F-FDG, thus 99m Tc-ECDG is not yet ideal 99m Tc-labeled DG imaging agent, with 18 F-FDG has a big gap

Method used

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  • Ligand compound for image diagnosis and its preparing method and compound for image diagnosis and its intermediate preparation
  • Ligand compound for image diagnosis and its preparing method and compound for image diagnosis and its intermediate preparation
  • Ligand compound for image diagnosis and its preparing method and compound for image diagnosis and its intermediate preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] 1) Mix 10ml SOCl with stirring 2 Add 3.94 g of diethylenetriaminepentaacetic acid (DTPA) (IV) dropwise at -30°C, and continue stirring at room temperature for 3 hours. The test results show that the temperature range of -30°C to 100°C in this process generally does not show significant adverse effects on the results. Then the reactant was refluxed for 20 hours, and the excess SOCl was evaporated under reduced pressure. 2 , to obtain 3.76 g of light yellow powder of the intermediate compound (III) of acid chloride bisanhydride, which can be directly carried out in the next step without separation.

[0030] 2) In the acid chloride bisanhydride 3.76g (0.010mol) obtained in the previous step, add 30ml DMSO, 5ml pyridine and 2.85g (0.0132mol) 2-amino-D-glucose hydrochloride, the mixture can generally be stirred at room temperature for 24 Hours (the operating temperature of this process can be allowed to be 20° C. to 150° C.), a transparent brown solution is obtained. The ...

Embodiment 2

[0049] In the acid chloride bisanhydride (0.010mol) obtained in the manner of Example 1, add 40ml DMSO, 8ml pyridine and 7.55g (0.035mol) 2-amino-D-glucose hydrochloride, and the mixture was stirred at 20°C to 140°C for 40 Hours, a transparent brown solution was obtained. This solution is separated and purified by dialysis membrane or dextran gel (G15), etc. to obtain R in the structure of formula (I). 1 , R 2 and R 3 Both are products of D-glucosamine-2 (DTPA-3DG).

[0050] Prepare with the resulting DTPA-3DG product 188 Refer to Example 1 for the method of Re-DTPA-3DG complex.

Embodiment 3

[0052] In the acid chloride bisanhydride (0.010mol) obtained in the manner of Example 1, add 30ml DMSO, 6ml pyridine and 2.35g (0.012mol) 2-mercapto-D-glucose, and the mixture was stirred at -10°C to 120°C for 40 hours, A brown solution was obtained. This solution is separated and purified by dialysis membrane or Sephadex (G10) to obtain R 1 is 2-mercapto-D-glucose, R 2 and R 3 All are the product of the formula (1) structure of H.

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Abstract

The invention relates to ligand compound used in image diagnosis and its preparation method, its intermediate compound, and the formed compound. R1 can be pentose, hexose, polysaccharide, or their deoxidizing structure. R2 and R3 can respectively be the above sugars and H. The preparation method is simple. And the cost is low. The formed ligand has ideal display effect. And its signed biology behavior is similar to DG, 18F-FDG. But its display cost is greatly reduced. It is exact molecule image checking medicine compound and is of great advantage to popularize and apply in tumor diseases early stage clinical diagnosis.

Description

technical field [0001] The present application relates to a complex compound for imaging diagnosis, a preparation method of the mixture, the corresponding compound for imaging diagnosis and an intermediate compound used for preparing the complex compound. Background technique [0002] Active glucose metabolism is an important metabolic feature of tumor cells. One of the main characteristics of malignant tumor cell metabolism is its increased glucose uptake and enhanced anaerobic glycolysis. The glucose analog 18-fluorodeoxyglucose ( 18 F-FDG) can be taken up by tumor cells, the tumor tissue 18 The distribution level of F-FDG is significantly higher than that of normal tissue and benign lesions around the tumor tissue. It is of great clinical significance to monitor the curative effect of various anticancer treatments and judge the prognosis of the disease. but 18 F-FDG PET (positron electron computed tomography) needs to be produced by cyclotron, which is costly and has...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K49/00C07H15/12C07H5/06C07D265/32
Inventor 何菱李举联陈跃郑时龙
Owner SICHUAN UNIV