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99mTc coordination compound, preparation method, intermediate and application thereof

A 99mtc and 99mtco4- technology, applied in the direction of radioactive carriers, can solve the problems of low labeling rate of diethylenetriaminepentaacetic acid, etc., and achieve the effects of excellent water solubility and stability, increased drug loading, and simple steps

Inactive Publication Date: 2012-10-03
SHANGHAI INST OF APPLIED PHYSICS - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0013] The technical problem to be solved by this invention is to overcome the existing Fac-[ 99m Tc(CO) 3 (H 2 O) 3 ]+ to the defect of low labeling rate of diethylenetriaminepentaacetic acid (DTPA), which provides a 99m Tc complex, its preparation method, intermediate and its application

Method used

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  • 99mTc coordination compound, preparation method, intermediate and application thereof
  • 99mTc coordination compound, preparation method, intermediate and application thereof
  • 99mTc coordination compound, preparation method, intermediate and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Example 1: Synthesis of compound V (n=77) (partial acetylation of the fifth generation polyamide-amine dendrimers)

[0052]

[0053] According to the literature (Istva'n J.Majoros, Acetylation of Poly(amidoamine) Dendrimers, Macromolecules 2003, 36, 5526-5529) acetylated dendrimers, the specific steps are as follows: 100mg of the fifth generation polyamide-amine dendrimers ( Compound VI, G5PAMAM, molecular weight 28824g / mol, stored in methanol, wt: 5%) (about 3.47 × 10 -6 mol), 24.9ul of glacial acetic acid (Ac 2 O) (about 2.43×10 -4 mol), 43.4ul of triethylamine (Et 3 N) (about 3.04×10 -4 mol) were mixed, stirred and reacted for 24 h at room temperature (25° C.) under nitrogen protection to obtain a colorless transparent liquid. Spin to dry the solvent, dissolve the product with deionized water, filter with a water-phase needle filter (specification 25mm×0.20um), and dialyze the filtrate in PBS solution (PBS formula: NaCl 8.0g, KCl 0.2g, NaCl 2 HPO 4 1.44g, K...

Embodiment 2

[0056] Example 2: Synthesis of Compound III (m=4, n=77) (Synthesis of PAMAM-Ac-Fa)

[0057]

[0058] 0.0116g of compound folic acid Fa (approximately 2.63×10 -5 mol), 0.0703g EDC·HCl, dissolved in 5ml of DMF / DMSO (3 / 1), mixed and reacted for 1h at room temperature (25°C) to activate the carboxyl group in folic acid. The solution was yellow. After 1h, add dissolved 3.27×10 -6 5ml DMSO solution of molPAMAM-Ac, reaction 3d. A yellow transparent solution was obtained. The solvent was spin-dried, and the product was dissolved in deionized water, filtered through a needle filter (25mm×0.20um) of the aqueous phase, and the filtrate was dialyzed in PBS solution for one day, and the PBS solution was replaced three times. The above product was continued to be dialyzed against deionized water for two days, changing the water three times a day. After dialysis, the obtained product was freeze-dried, and the yield was about 90.3%.

[0059] Its identification data are as follows:

...

Embodiment 3

[0061] Example 3: Synthesis of Compound I (m=4, n=77) (Synthesis of PAMAM-Ac-Fa-DTPA)

[0062]

[0063] In containing PAMAM-Ac-Fa about 2.94×10 -6 mol aqueous solution was added 0.0572gDTPA (about 1.03×10 -4mol), adjust the pH value to about 9 with NaOH solution, and react at 40°C for 24h to obtain a yellow transparent solution. The solvent was spin-dried, and the product was dissolved in deionized water, filtered through a needle filter (25mm×0.20um) of the aqueous phase, and the filtrate was dialyzed in PBS solution for one day, and the PBS solution was replaced three times. The above product was continued to be dialyzed against deionized water for two days, changing the water three times a day. After dialysis, the obtained product was freeze-dried, and the yield was about 92.7%. Carry out HPLC analysis to it, the result sees attached figure 1 , retention time t=10.825min.

[0064] The NMR data are as follows:

[0065] 1 H-NMR (D 2 O, TMS, 500MHz), δ1.88 (230H, s)...

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Abstract

The invention discloses a 99mTc coordination compound shown as a formula II, wherein m is equal to 1-10; n is equal to 60-85; and a spherical structure refers to a structure in a polyamide-amine dendrimer macromolecule except 128 -NH2. The invention also discloses a preparation method, an intermediate and application thereof. The 99mTc coordination compound has tumor targeting and high water solubility and stability, and is a single photon emission computed tomography (SPECT) developer with higher metabolic capacity.

Description

technical field [0001] The present invention relates to a radioactive metal complex, its preparation method, an intermediate and its application, in particular to a 99m Tc complexes, their preparation methods, intermediates and their applications. Background technique [0002] Single-Photon Emission Computed Tomography (SPECT) is a nuclear medicine computed tomography technique using gamma rays. SPECT uses traditional nuclear medicine contrast agent (radiotracer) and Angle gamma camera to surround the target organ of the patient at a certain angle to obtain a series of planar images, and obtain another series of images by computer image reconstruction technology, thus obtaining Transaxial, Stereoscopic image of Sagittal, Coronal. [0003] The basic imaging principle of SPECT: General nuclear medicine seeds are produced by generators, such as: Tc-99m, I-131, I-125. Most of this type of nuclei have too many neutrons, so during the production process, neutrons are used to hi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G69/48C08G73/02A61K51/06A61K103/10
Inventor 沈玉梅张元庆孙艳红许晓平
Owner SHANGHAI INST OF APPLIED PHYSICS - CHINESE ACAD OF SCI
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