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<99>Tc<m>N(NFXDTC)2 complex and preparation method and application thereof

A 99tcmn, complex technology, applied in the field of 99TcmN2 complex and its preparation, can solve problems such as low inflammation/muscle ratio

Active Publication Date: 2010-03-10
BEIJING NORMAL UNIVERSITY +1
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

and 99 Tc m -ciprofloxacin compared to 99 Tc m Although N-CPFXDTC has high inflammation uptake and inflammation / blood ratio, its inflammation / muscle ratio is low, so it is still necessary to develop a more ideal new inflammation imaging agent in this technical field

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  • &lt;99&gt;Tc&lt;m&gt;N(NFXDTC)2 complex and preparation method and application thereof

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Embodiment Construction

[0048] Describe the present invention in detail below by embodiment, a kind of 99 Tc m N(NFXDTC) 2 Preparation of complexes, including:

[0049] a. Synthesis of Ligand NFXDTC:

[0050] Under ice-water bath cooling, add 0.08g NaOH dissolved in cold aqueous solution to 0.319g norfloxacin (0.001mol), cool to 5°C in ice-water bath, add dropwise 3-4 drops of CS 2 , Stir the reaction under cooling for 2 h, then stir and react at room temperature overnight. After the reaction was completed, water was removed by rotary evaporation to obtain a yellow solid, which was recrystallized from methanol / anhydrous ether to obtain 0.365 g of a light yellow solid with a yield of 83%. Product NFXDTC through IR, 13 CNMR and ESI-MS identification.

[0051] IR (KBr, cm -1 ): 3414 (vOH), 1626 (vC=O), 1010 (vC=S).

[0052] 13 CNMR (D 2 O, δ): 209.4, 175.2, 172.9, 146.5, 144.1, 144.0, 136.8, 117.7, 111.9, 111.7, 106.2, 50.48, 49.7, 49.2, 13.6.

[0053] ESI-MS(m / z): 394[M-2Na+H] - , 100%

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Abstract

The invention discloses a <99>Tc<m>N(NFXDTC)2 complex and a preparation method and an application thereof, the complex comprises an irregular square pyramid geometric configuration and takes a <99>Tc<m>N nucleus as a central nucleus, wherein, an N atom in a Tc equivalent to N triple bond is positioned in the vertex position, and four sulfur atoms provided by two ligand NFXDTC molecules are positioned at four points of the bottom surface. The <99>Tc<m>N(NFXDTC)2 complex has the advantages of high radiochemical purity, good stability, higher uptake value of inflammation and better target / non-target value and is convenient to popularize and apply as a novel inflammation imaging agent.

Description

Technical field [0001] The present invention relates to 99 Tc m The field of nuclear-labeled radiopharmaceutical chemistry and clinical nuclear medicine technology, specifically related to a 99 Tc m N(NFXDTC) 2 Compounds and their preparation methods and applications. Background technique [0002] Nuclide inflammation imaging is an important method for early detection of lesions. Inflammation imaging agents can be divided into proteins, antibiotics, leukocytes, and small molecule compounds according to different markers. The nuclides used are as follows: 67 Ga, 111 In and 99 Tc m . 99 Tc m Excellent nuclear properties, cheap and easy to obtain and other advantages make it one of the preferred nuclides for radiopharmaceutical research. 99 Tc m Labeled white blood cell imaging can detect acute and chronic inflammatory lesions, known as the "gold standard", but the labeling process is complicated and cross-infection is prone to occur, so its clinical application is l...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F13/00C07D215/56A61K51/04A61K103/10
Inventor 张俊波张仕坚王跃王学斌唐志刚张现忠陆洁
Owner BEIJING NORMAL UNIVERSITY
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