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Evans blue complex as well as preparation method and application thereof

An Evans blue and complex technology, applied in the field of radioactive complexes, can solve the problems of susceptible virus imaging effect, susceptible to other factors, complicated preparation method, etc. Effect

Active Publication Date: 2013-08-14
厦门锐谱思科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] It can be seen from this that the existing relatively successful blood pool imaging agents are limited to technetium-99m-labeled red blood cells or radiolabeled biological extract HSA, and there are still complex preparation methods, high prices, easy virus infection, and imaging effects. Susceptible to other factors and other shortcomings, if a new type of radiolabeled blood pool imaging agent with the characteristics of simple preparation, low cost and good imaging effect can be provided, it will have broad application prospects

Method used

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  • Evans blue complex as well as preparation method and application thereof
  • Evans blue complex as well as preparation method and application thereof
  • Evans blue complex as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] 1. Preparation of Evans Blue Derivative Ligand (Compound 6)

[0072] 1) Synthesis of Compound 3:

[0073] Mix and dissolve 20.0 mg of compound 1 (ortho-dimethylbenzidine, 94 μmol) and 20.0 mg of compound 2 (NOTA-3HCl, 48 μmol) in 1 mL of DMSO, then add 3.6 μL of diethyl cyanophosphate (24 μmol) and 25 μL Diisopropylethylamine (DIPEA) was added to the above mixture, and after stirring at room temperature for 40 min, 3.6 μL of diethyl cyanophosphate (24 μmol) was added again, and the reaction mixture was kept stirring overnight at room temperature. The product (compound 3) was separated and purified by semi-preparative HPLC, and the fraction with a retention time of 10.0 min was collected and freeze-dried to obtain about 12.2 mg of pure compound 3 with a yield of 26.4%. The intermediate product was identified by liquid chromatography-mass spectrometry (LC-MS): [MH] + =498.2462, the calculated value (m / z) is 497.2638 (C 26 h 35 N 5 o 5 ).

[0074] 2) Synthesis of Co...

Embodiment 2

[0077] 1. radioactivity 18 Preparation of F-marked freeze-dried kit (take the preparation of 100 tubes as an example)

[0078] Weigh 8 mg of compound 6 and dissolve in 10 mL of 0.5 mol / L acetic acid-sodium acetate buffer solution (pH4), then add 0.08 mg of aluminum chloride (AlCl 3 ) was dissolved in 10mL of 0.5mol / L acetic acid-sodium acetate buffer solution (pH4), and the two were evenly mixed. After sterile filtration, it is divided into 100 control antibiotic vials, then placed in a freeze dryer for 24 hours, and then sealed with a stopper to obtain a freeze-dried medicine box. According to the output of the kit and the requirements for the content of the components in each kit, the amount of compound 6 and aluminum chloride can be adjusted so that their weight ratio falls within the range of (20-100):1.

[0079] 2. 18 Preparation of F-labeled Evans blue complex (compound 7):

[0080] 1) Wet method: In a 1mL plastic tube, add 3μL of 2mM AlCl 3 Acetic acid-acetate buf...

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Abstract

The invention discloses an Evans blue complex as well as a preparation method and application thereof. The Evans blue complex structurally contains macrocylic polymine chelation groups NOTA. A marker complex is obtained after marking by using radionuclides (Fluorine-18, copper-64, gallium-68 and the like). The marker complex is prepared by using a wet process or a lyophilisation method. The invention further relates an application of the complex as a developer in organs or tissues of human or animals, and especially a blood pool developer. The Evans blue complex has the advantages of low cost and higher target-to-nontarget ratio, and is simple to prepare.

Description

technical field [0001] The invention relates to a class of radioactive complexes, a preparation method thereof and the application of the complexes as blood pool imaging agents. Background technique [0002] Vascular system diseases seriously affect human health. It is necessary to effectively display blood vessels by imaging means and combine immunohistochemical research to explore the pathogenesis of diseases. At present, the commonly used vascular imaging methods include ink perfusion, immunohistochemistry, tannic acid mordant staining, enzyme histochemistry and so on. However, these methods have their own disadvantages, such as not being able to combine with immunohistochemical research, the process is cumbersome or the fluorescence is easily quenched. [0003] The use of radionuclide-labeled imaging agents to image the vascular system is one of the hotspots in radiopharmaceutical research today. Radionuclide blood pool imaging can non-invasively measure local or overa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D255/02C07F5/06C07F1/08C07F5/00A61K51/04A61K101/02
Inventor 张现忠陈小元郎立新牛刚李方朱朝晖
Owner 厦门锐谱思科技有限公司
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