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99mTc complex, preparation method, intermediate and application thereof

A 99mtc, 99mtco4- technology, applied in the direction of radioactive carriers, can solve the problem of low labeling rate, achieve the effect of simple steps, good imaging prospect, and enhanced imaging effect

Inactive Publication Date: 2012-08-22
SHANGHAI INST OF APPLIED PHYSICS - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] The technical problem to be solved by this invention is to overcome the existing Fac-[ 99m Tc(CO) 3 (H 2 O) 3 ] + For the defect of low labeling rate of diethylenetriaminepentaacetic acid bifunctional chelating agents, it provides a 99m Tc complex, its preparation method, intermediate and its application

Method used

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  • 99mTc complex, preparation method, intermediate and application thereof
  • 99mTc complex, preparation method, intermediate and application thereof
  • 99mTc complex, 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 Fifth Generation Polyamido-amine Dendrimers)

[0052]

[0053] According to the literature (Istva'n J.Majoros, Acetylation of Poly(amidoamine) Dendrimers, Macromolecules 2003,36,5526-5529) acetylation dendrimers, the specific steps are as follows: 100mg fifth generation polyamide-amine dendrimers (compound Ⅵ, G5PAMAM, molecular weight 28824g / mol, stored in methanol, wt: 5%) (about 3.47×10 -6 mol), 24.9μl acetic anhydride (Ac 2 O) (about 2.43×10 -4 mol) and 43.4μl 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, and a colorless transparent liquid was obtained. Spin to dry the solvent, dissolve the product with deionized water, filter with a water-phase needle filter (specification 25mm×0.20μm), and dialyze the filtrate in PBS solution (PBS formula: NaCl 8.0g, KCl 0.2g, NaCl 2 HPO 4 1.44g, KH 2 PO 4 0.27...

Embodiment 2

[0056] Example 2: Synthesis of Compound III (m=7, n=77, p=10) (Synthesis of PAMAM-Ac-pegFa)

[0057]

[0058] 0.090g compound VII (about 3.27×10 -5 mol) was dissolved in 3ml DMSO, at 15°C, a solution of 3.27×10 -6 mol PAMAM-Ac in 3ml DMSO solution, 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 (25 mm×0.20 μm) 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 in deionized water for two days, and the deionized water was changed three times a day. After the dialysis, the obtained product was freeze-dried, and the yield was about 93.7%.

[0059] Its identification data are as follows:

[0060] 1 H-NMR (D 2 O, TMS, 500MHz), δ1.89(230H, s), 2.28(504H, s), 8.64(7H), 7.62(14H), 6.68(14H)

Embodiment 3

[0061] Example 3: Synthesis of Compound I (m=7, n=77, p=10) (Synthesis of PAMAM-Ac-pegFa-DTPA)

[0062]

[0063] containing approximately 2.94 x 10 -6 mol PAMAM-Ac-pegFa (compound III) in the aqueous solution (5mL), add 0.0572g compound IV (about 2.94×10 -5 mol), adjust the pH value to about 9 with NaOH solution (1M). At 40°C, reacted 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 (25 mm×0.20 μm) 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 in deionized water for two days, and the deionized water was changed three times a day. After the dialysis, the obtained product was freeze-dried, and the yield was about 94.4%.

[0064] The NMR data are as follows:

[0065] 1 H-NMR (D 2O, TMS, 500MHz), δ1.88 (230H, s), 2.33 (504H, s), 6.78 (...

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Abstract

The invention discloses a 99mTc complex as shown in formula II; wherein m=1-10, n=60-85, p=10-50; a globular structure represents a structure in a polyamidoamine dendrimer except 128 -NH2. The invention also discloses a preparation method, an intermediate and an application thereof. The 99mTc complex of the invention has excellent tumor targeting, water solubility, and stability, and is a SPECT developer with good metabolic capability.

Description

technical field [0001] The present invention relates to a radioactive metal complex, its preparation method, 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. [0003] 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 then obtain another series of images by computer image reconstruction technology, thus obtaining Transaxial, Stereoscopic images of Sagittal and Coronal. [0004] The basic imaging principle of SPECT: General nuclear medicine seeds are produced by generators, such as Tc-99m, I-131 or I-125. Most of the nuclei of this type belong to the neutron-excessive type. During the production p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G69/48A61K51/06A61K103/10
Inventor 沈玉梅张元庆许晓平孙艳红杨光崔巍朱华
Owner SHANGHAI INST OF APPLIED PHYSICS - CHINESE ACAD OF SCI
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