Aspartate-leucine copolymer modified paramagnetism metal complex as well as preparation method and application thereof

A technology of leucine copolymer and paramagnetic metal, which is applied in the field of paramagnetic metal complexes and its preparation, can solve the problems of high dosage and low targeting of magnetic resonance contrast agents, and achieve low dosage and stable aqueous solution sex, reducing the effect of accumulation

Inactive Publication Date: 2016-09-28
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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Problems solved by technology

[0005] The purpose of the present invention is to solve the technical problems of low targeting and high dosage of magnetic resonance contrast agents in the prior art, further improve the relaxation efficiency, imaging contrast, clarity and sensitivity of contrast agents, and provide a kind of aspartic acid Acid-leucine copolymer modified paramagnetic metal complex and its synthesis method and application

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  • Aspartate-leucine copolymer modified paramagnetism metal complex as well as preparation method and application thereof
  • Aspartate-leucine copolymer modified paramagnetism metal complex as well as preparation method and application thereof
  • Aspartate-leucine copolymer modified paramagnetism metal complex as well as preparation method and application thereof

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preparation example Construction

[0047] The preparation method of the paramagnetic metal complex modified by the above-mentioned aspartic acid-leucine copolymer, the steps are as follows:

[0048] Step 1. Mix aspartic acid, leucine and concentrated phosphoric acid evenly in molar ratios to obtain a mixture. Heat the mixture on a rotary evaporator. When the temperature rises to 150°C, vacuumize until the vacuum degree is less than -1.0MPa. Then heat to 160-200°C and react for 2-6 hours; after the reaction, add DMF to the reaction liquid, then pour the system into distilled water, filter with suction, and dry in vacuum to obtain aspartic acid-leucine copolymer. The structural formula is as follows:

[0049]

[0050] In the formula, x, y and m are natural numbers;

[0051] Wherein, the concentration of concentrated phosphoric acid is not particularly limited, is generally 85%, and the molar ratio of phosphoric acid in aspartic acid, leucine and concentrated phosphoric acid is 1:(0.001-1000):(0.1-10), DMF is ...

Embodiment 1

[0067] Preparation of gadolinium complexes of diethylenetriaminepentaacetate modified by aspartic acid-leucine copolymer:

[0068] Step 1. Mix 7.03g of aspartic acid, 2.97g of leucine and 5ml of 85% phosphoric acid solution evenly, heat the obtained mixture on a rotary evaporator, and vacuumize it when the temperature rises to 150°C until the vacuum degree is less than - 1.0MPa, heated to 185°C, and reacted for 4 hours; after the reaction, add 50ml DMF to the reactant, then pour the mixture into 200ml distilled water, filter with suction, and dry in vacuum to obtain aspartic acid-leucine copolymer .

[0069] Step 2, 2.0 g of aspartic acid-leucine copolymer synthesized in step 1 and 24 ml of ethylenediamine were dissolved in 24 ml of DMF respectively to obtain aspartic acid-leucine copolymer solution and ethylenediamine solution , under the condition of ice-water bath, add the aspartic acid-leucine copolymer solution dropwise into the ethylenediamine solution, react for 2.5 ho...

Embodiment 2

[0074] Preparation of gadolinium complexes of diethylenetriaminepentaacetate modified by aspartic acid-leucine copolymer:

[0075]Step 1. Mix 7.03g of aspartic acid, 2.97g of leucine and 5ml of 85% phosphoric acid solution evenly, heat the obtained mixture on a rotary evaporator, and vacuumize it when the temperature rises to 150°C until the vacuum degree is less than - 1.0MPa, heated to 160°C, and reacted for 2 hours; after the reaction, add 50ml DMF to the reactant, then pour the mixture into 200ml distilled water, filter with suction, and dry in vacuum to obtain aspartic acid-leucine copolymer .

[0076] Step 2, 2.0 g of aspartic acid-leucine copolymer synthesized in step 1 and 24 ml of ethylenediamine were dissolved in 24 ml of DMF respectively to obtain aspartic acid-leucine copolymer solution and ethylenediamine solution , under the condition of ice-water bath, add the aspartic acid-leucine copolymer solution dropwise into the ethylenediamine solution, after reacting fo...

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Abstract

The invention discloses an aspartate-leucine copolymer modified paramagnetism metal complex as well as a preparation method and application thereof, belongs to the technical field of contrast agents, and solves the technical problems in the prior art that a magnetic resonance contrast agent is lower in targeting and high in dosage so as to further improve the relaxation efficiency, imaging contrast ratio, definition and sensitivity of the contrast agent. The structural formula of the metal complex is shown in the formula I (refer to the description), wherein z is an integer ranging from 1 to 1000, x is an integer ranging from 1 to 1000, y is an integer ranging from 1 to 1000, and M<m+> refers to paramagnetism metal ions. The metal complex can be used as a magnetic resonance imaging contrast agent which has excellent stability, water-solubility and relaxation efficiency, also has excellent targeting to a liver, and is higher in imaging contrast ratio and definition; the dosage lower limit of the metal complex is only 0.001 mmol/kg.

Description

technical field [0001] The invention belongs to the technical field of contrast agents, and in particular relates to a paramagnetic metal complex modified by an aspartic acid-leucine copolymer and a preparation method and application thereof. Background technique [0002] Magnetic resonance imaging (magnetic resonance imaging, MRI) technology is another medical imaging technology after X-ray CT. Magnetic resonance imaging technology can image organisms from various angles, has very high temporal resolution and spatial resolution, and can present complete and clear anatomical images, and has been widely used in clinical diagnosis. [0003] Magnetic resonance imaging contrast agents are compounds used to shorten imaging time, enhance contrast, and improve imaging contrast and clarity. About 50% of magnetic resonance imaging requires the use of magnetic resonance imaging contrast agents. MRI contrast agents do not generate signals by themselves, but improve the imaging contras...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/14
CPCA61K49/146
Inventor 李晓晶祝云龙湛游洋万传玲薛蓉裴奉奎
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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