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<19>F nuclear magnetic resonance probe, preparation method and applications thereof

A technology of nuclear magnetic resonance and probes, which can be used in peptide preparation methods, chemical instruments and methods, and pharmaceutical formulations, and can solve problems such as inability to reflect tumor-related conditions

Inactive Publication Date: 2018-08-21
SOUTHERN MEDICAL UNIVERSITY
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  • Abstract
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Problems solved by technology

[0004] However, only the in vivo detection of cathepsin B activity expression can reflect the possible tumors related to it, and the in vitro detection technology cannot reflect the relevant conditions of the tumor.

Method used

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  • &lt;19&gt;F nuclear magnetic resonance probe, preparation method and applications thereof
  • &lt;19&gt;F nuclear magnetic resonance probe, preparation method and applications thereof
  • &lt;19&gt;F nuclear magnetic resonance probe, preparation method and applications thereof

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Embodiment 1

[0047] 19 Preparation of F NMR probes

[0048] 19 The preparation method of F nuclear magnetic resonance probe, such as Figure 1~6 shown, including the following steps:

[0049] 1) Synthesis of 2-cyano-6-aminobenzothiazole (CBT)

[0050] Under the condition of wt 98% concentrated sulfuric acid, 10 mmol 2-chlorobenzothiazole was reacted with 10 mmol potassium nitrate to generate 10 mmol 2-chloro-6-nitrobenzothiazole. Under the conditions of glacial acetic acid, water, ethanol, reduced iron powder, and activated carbon, the mixed solution of ethanol and water is the reaction solvent, and the dosage is 20 mL of ethanol, 20 mL of pure water, and the reduced iron powder and activated carbon are the catalysts of the reaction, and the dosage is iron Powder 0.01g, activated carbon 0.01g, 20mmol glacial acetic acid and 10mmol 2-chloro-6-nitrobenzothiazole were reacted to obtain 10mmol 2-chloro-6-aminobenzothiazole. Anhydrous N,N-dimethylformamide (DMF) is used as a reaction solve...

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Abstract

The present invention provides a novel fluorine-containing <19>F nuclear magnetic resonance probe, which has a chemical formula of C49H58F6N10O7S3, has the following structural formula defined in thespecification, and can be used for detecting cathepsin B. According to the present invention, the magnetic resonance signal of the <19>F nuclear magnetic resonance probe is proportional to the activity of cathepsin B in vivo, the stronger the signal, the higher the activity of the cathepsin B, and the signal exceeding a certain threshold is related to malignant tumors, such that the new technicalway is provided for the early detection of tumors.

Description

technical field [0001] The present invention relates to the technical field of nuclear magnetic resonance probes, more specifically, to a 19 F nuclear magnetic resonance probe and its preparation method and application. Background technique [0002] The incidence of tumors in today's society is getting higher and higher, and the prevention and early diagnosis of tumors has become a research hotspot. Especially malignant tumors have the highest fatality rate. If they can be diagnosed and prevented early, malignant tumors can be killed in the bud. Studies have found that cathepsin B is highly expressed in the early stages of various malignant tumors, such as lung cancer, gastric cancer and prostate cancer. If the abnormally high expression of cathepsin B in the body can be detected in time, cancer can be found in the first place. [0003] At present, the detection methods of cathepsin B mainly include fluorescence method, chromogenic substrate method, indirect method and nu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C09K11/06C07K7/06C07K1/16C07K1/06C07K1/04A61K49/14
CPCA61K49/14C07K7/06C09K11/06C09K2211/1007C09K2211/1037
Inventor 张蒙张翠兰余学飞李喆张宁罗敏敏王丹丹郭淑艳
Owner SOUTHERN MEDICAL UNIVERSITY
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