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Positron nuclide labeled selenocysteine compound and application thereof

A technology of selenocysteine ​​and compound is applied in the application field of preparing positron emission tomography imaging agent, and the effect of good development prospect is achieved

Inactive Publication Date: 2014-10-08
广州市原子高科同位素医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] So far, there is no precedent for the application of positron-nuclides-labeled selenocysteine ​​analogues as positron emission tomography (PET) imaging agents

Method used

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  • Positron nuclide labeled selenocysteine compound and application thereof
  • Positron nuclide labeled selenocysteine compound and application thereof
  • Positron nuclide labeled selenocysteine compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 111

[0037] Example 1 11 Radiosynthesis of C-SeMCYS

[0038] 1 Materials and Instruments

[0039] 1.1 Main reagents and consumables. Kryptofix2.2.2 (K222), anhydrous acetonitrile, anhydrous K 2 CO 3 , lithium aluminum hydride, USP ethanol, 1.0N hydrochloric acid, dimethyl sulfoxide, and 1,3-propanediol-di-p-toluenesulfonate, products of Sigma-Aldrich Company in the United States; L-selenocysteine, domestic purchase; 18 O-H 2 O, ABX Company; Iodomethane, Sinopharm Chemical Reagent Co., Ltd.; Chloral hydrate, prepared by the First Affiliated Hospital of Sun Yat-sen University. Silica gel60TLC alumimium sheets5×10cm, Merck, Germany; Sep Pak Plus C18 column, Sep Pak light QMA column, Sep Pak plus SiO2 column, Sep Pak light CM column, Sep Pak Plus tC18 column, Water s, USA Product; Sep Pak SCX small column, product of Alltech Company in the United States.

[0040] 1.2 Main experimental instruments. Cyclone10 / 5 medical cyclotron, Belgian IBA company; PET-CS-II-IT-I carbon-11 met...

Embodiment 218F

[0050] Example 2 18 F-labeled selenocysteine ​​compounds 18 Synthesis of F-SeFPCYS

[0051] 2.1 18 F-labeled selenocysteine ​​compounds 18 Synthesis of F-SeFPCYS

[0052] cyclotron through nuclear reaction 18 O(p,n) 18 F production gets 18 f - , after capture by QMA, with 1.0mL of K222 / K 2 CO 3 solution elution 18 f - into the reaction tube, feed N at 108°C 2 The solvent was evaporated to dryness. Then add 0.5 mL of anhydrous acetonitrile and evaporate to dryness, repeat three times. In the dry K222 solution, add propylene glycol 1,3-di-p-toluenesulfonate (TsOCH 2 CH 2 CH 2 OTs)7.7mg (0.02mmol) of anhydrous acetonitrile (1.0mL) solution, N 2 React at 90°C for 10 minutes under protection. After directly evaporating to dryness, a solution of 3.3 mg (0.02 mmol) of precursor L-selenocysteine ​​dissolved in DMSO (0.5 mL) and 20 μL of 10% NaOH solution were added, and reacted at the same temperature for 5 min. Add 5mL of water, rinse the silica gel column with 5mL...

Embodiment 318

[0056] Example 3 18 Synthesis of F-SeFECYS

[0057] With the 1,3-dipropylene glycol tosylate (TsOCH 2 CH 2 CH 2 OTs) in anhydrous acetonitrile (1.0 mL) was replaced by 1,2-diethylene sulfonate (TsOCH 2 CH 2 OTs), all the other are with embodiment 2, make 18 F-SeFECYS Injection.

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Abstract

The invention relates to a Se-substituted positron nuclide labeled L-selenocysteine compound. The general structure formula of the Se-substituted positron nuclide labeled L-selenocysteine compound is shown in the specification, wherein R* represents for -11CH3, -CH218F, -CH2CH218F, -CH2CH2CH218F. Positron nuclide (11C or 18F) is labeled in the position of -Se in L-selenocysteine so as to form a novel Se-substituted positron nuclide labeled L-selenocysteine compound. A preparation method of the labeled selenocysteine compound is simple and capable of easily achieving automatic synthesis. The labeled selenocysteine compound is highly absorbed in the tumor tissue. The invention also relates to application of the selenocysteine compound in preparation of a positron emission tomography (PET) photographic developer; the selenocysteine compound can be used for identifying and diagnosing tumor, monitoring the curative effect of the anti-tumor treatment, diagnosing cardiovascular and cerebrovascular diseases and monitoring curative effect of treatment of the cardiovascular and cerebrovascular diseases.

Description

technical field [0001] The invention relates to a selenocysteine ​​positron emission tomography (PET) imaging agent, its preparation method and its application in preparing the positron emission tomography (PET) imaging agent. Background technique [0002] Selenium is an essential trace element that has an important impact on human health. In organisms, it exists in the form of organic compounds and mainly in the form of selenoproteins or selenoenzymes (such as glutathione peroxidase, thyroxine 5-deiodinase, etc.), selenocysteine ​​(selenocysteine) , SeCYS) is the main selenoamino acid that constitutes these selenoproteins or selenoenzymes (Bhattacharya A. Methylselenocysteine-a promising antiangiogenic agent for overcoming drug delivery barriers in solid malignancies for therapeutic synergy with anticancer drugs. Expert Opin Drug Deliv, 2011, 8( 6): 749-763). The structure of SeCYS is similar to that of cysteine, except that the sulfur atom is replaced by selenium. SeCYS...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C391/00A61K51/04
Inventor 唐刚华
Owner 广州市原子高科同位素医药有限公司
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