<99m>tc complex, and 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, excellent water solubility and stability, and overcome poor water solubility

Inactive Publication Date: 2013-07-03
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

[0010] The technical problem to be solved by this invention is: in order to overcome existing Fac-[ 99m Tc(CO) 3 (H 2 O) 3 ] + For the defect of low labeling rate of diethylenetriaminepentaacetic acid bifunctional chelating agent, a kind of 99m Tc complex, its preparation method, intermediate and its application

Method used

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  • &lt;99m&gt;tc complex, and preparation method, intermediate and application thereof
  • &lt;99m&gt;tc complex, and preparation method, intermediate and application thereof
  • &lt;99m&gt;tc complex, and preparation method, intermediate and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1: Synthesis of Compound V (n=81) (Partial Acetylation of Fifth Generation Polyamidoamine Dendrimer)

[0049]

[0050] 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 of the fifth generation polyamide-amine dendrimers ( Compound VI, G5 PAMAM, molecular weight 28824, stored in methanol, wt: 5%) (approximately 3.47×10 -6 mol), 24.9 μl of acetic anhydride (Ac 2 O) (about 2.43×10 -4 mol) and 43.4 μl 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, 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....

Embodiment 2

[0053] Example 2: Synthesis of Compound III (m=9, n=81) (Synthesis of PAMAM-Ac-Bt)

[0054]

[0055] 30mg biotin (1.24×10 -4 mol), 48mg EDC·HCl (2.48×10 -4 mol) and 36mgHOBt (2.48×10 -4 mol) was dissolved in 2ml DMSO, reacted at room temperature for 1h, then added 5ml dissolved in 100mg partially acetylated fifth-generation polyamido-amine dendrimers (G5-Ac, 3.1×10 -6 mol) in DMSO solution, reacted at room temperature for 1 d, diluted with deionized water, filtered to remove unreacted biotin, and the filtrate was dialyzed in PBS solution for one day, and the PBS solution was changed 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%.

[0056] Its identification data are as follows:

[0057] 1 H-NMR (D 2 O, TMS, 500MHz), δ1.88 (244H, s), 2.33 (504H, br), 4.44 (9H, s), 4.62 (10H, s)

Embodiment 3

[0058] Example 3: Synthesis of Compound I (m=9, n=81, p=10) (Synthesis of PAMAM-Ac-Bt-DTPA)

[0059]

[0060] incl. 3 x 10 -6 mol G5-Ac-Bt aqueous solution (concentration 0.6mM), add 6×10 -5 mol of compound IV, adjust pH=9 with 1M NaOH solution, react at 40°C for 24 hours, dilute with deionization, filter with an aqueous needle filter (size 25mm×0.20μm), dialyze the filtrate in PBS solution for one day, replace PBS solution 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%.

[0061] The NMR data are as follows:

[0062] 1 H-NMR (D 2 O, TMS, 500MHz), δ1.88(244H, s), 2.33(504H, br), 4.44(9H, s), 4.62(10H, s), 6.84(18H, m), 7.11(21H, m)

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Abstract

The invention discloses a <99m>Tc complex as represented by formula II, wherein, m = 5 to 20, n = 60 to 90, p = 5 to 20, and a spherical structure means a structure of polyamidoamine dendrimer free of 128 -NH2s. The invention also discloses a preparation method, an intermediate and application of the complex. The <99m>Tc complex provided in the invention has excellent tumor targeting, water-solubility and stability, and is an SPECT (single-photon emission computed tomography) developer with good metabolic capability.

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 then obtain another series of images by computer image reconstruction technology to obtain Transaxial, Sagittal , Stereoscopic image of 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 are neutron-excessive. In the process of production, neutrons are used to hit th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G69/48A61K51/06A61K103/10
Inventor 沈玉梅许晓平张元庆朱华王旭东
Owner SHANGHAI INST OF APPLIED PHYSICS - CHINESE ACAD OF SCI
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