Fluorine-18 marked sugar-based amino acid compound, as well as preparation method and application thereof

A technology of amino acids and compounds, applied in the fields of radiopharmaceutical chemistry and clinical nuclear medicine, to achieve the effect of good biological properties, wide sources and easy access

Active Publication Date: 2017-05-17
上海释雅医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, 18F-FDG PET molecular imaging has an irreplaceable advantage in the diagnosis and treatment of tumors in the clinic. The development of multiple metabolic dual-targeted drugs that retain the effective functional groups of 18F-FDG and can also realize the diagnosis of amino acid metabolism will help improve the efficiency of tumor diagnosis, It is of great significance to reduce the occurrence of missed diagnosis and misdiagnosis, and to avoid the increase of radiation dose caused by multiple PET imaging

Method used

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  • Fluorine-18 marked sugar-based amino acid compound, as well as preparation method and application thereof
  • Fluorine-18 marked sugar-based amino acid compound, as well as preparation method and application thereof
  • Fluorine-18 marked sugar-based amino acid compound, as well as preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0026] Embodiment 1: wet preparation [ 18 F] The preparation method of FDGlyNHPHe is as follows:

[0027] 0.5mL of 37MBq 18 F-FDG injection is placed in a closed container, 2 mL of acetonitrile is added twice, azeotropically dried under negative pressure, and then a mixture of 1.0 mg of p-aminophenylalanine in methanol and water (0.5 mL of methanol and 0.05 mL of water) and 50 μl of acetic acid, the container was sealed and reacted at 100° C. for 30 min; finally, the reaction solution was directly purified by preparative high-performance liquid chromatography. The conditions of preparative high performance liquid chromatography are: amino preparative column (250mm×10mm), mobile phase methanol:water=9:1, 3mL / min, UV=254nm. Collect the fractions between 10-17min, evaporate the solution to dryness, add PBS or normal saline, and then dilute and dissolve to obtain [ 18 F] The injection of FDGlyNHPHe is used after passing through a sterile filter membrane.

Embodiment 2

[0028] Embodiment 2: dry preparation [ 18 F] The preparation method of FDGlyNHPHe is as follows:

[0029] 0.5mL of 37MBq 18 Put F-FDG injection in a closed container, add 1.0mg of p-aminophenylalanine and 50μl of acetic acid at the same time, add 2mL of acetonitrile in two times, and azeotropically dry under negative pressure. After the solution is evaporated to dryness, the container is sealed. The reaction was carried out at 80° C. for 30 min; finally, the reaction solution was directly purified by preparative high performance liquid chromatography. The conditions of preparative high performance liquid chromatography are: amino preparative column (250mm×10mm), mobile phase methanol:water=9:1, 3mL / min, UV=254nm. Collect the fractions between 10-17min, evaporate the solution to dryness and add PBS to dilute and dissolve to obtain [ 18 F] The injection of FDGlyNHPHe is used after passing through a sterile filter membrane.

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Abstract

The invention discloses a fluorine-18 marked sugar-based amino acid compound, as well as a preparation method and application thereof. The chemical expression of the compound is [18F]FDGlyNHPHe. The fluorine-18 marked sugar-based amino acid compound is prepared by carrying out a reaction of radioactive 2-[18F]F-fludeoxyglucose ([18F]-FDG) and p-aminophenylalanine (NH2PHe) under the acidic condition. The compound has high chemical stability, high biological property and high chemical purity, is simple to prepare, has the advantages of high tumor intake, low inflammation intake, and good target / nontarget ratio of tumor / muscle, tumor / blood, tumor / brain, tumor / heart, tumor / inflammation and the like, and is a novel tumor imaging agent with popularization and application value.

Description

technical field [0001] The invention relates to a fluorine-18 labeled glycosyl amino acid compound and its preparation method and application, belonging to the fields of radiopharmaceutical chemistry and clinical nuclear medicine. Background technique [0002] Positron emission tomography (PET) technology is an important means of tumor diagnosis based on the molecular level, and has been widely used and affirmed in clinic. 2-[18F]-Fluorodeoxyglucose (18F labeled 2-fluoro-2-deoxy-D-glucose, 18F-FDG) is currently the most widely used clinically and irreplaceable PET imaging agent for tumor glucose metabolism. However, there are still some limitations in the clinical application of 18F-FDG in the imaging of brain tumors with glucose metabolism as the energy substrate and the differential diagnosis of tumors and inflammation. In order to improve the efficiency and specificity of tumor diagnosis and reduce the rate of missed diagnosis, many scholars are constantly looking for an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/203C07H1/00A61K51/04A61K101/02
CPCA61K51/0491C07H1/00C07H15/203
Inventor 武志芳王红亮马晶鑫李思进解军
Owner 上海释雅医药科技有限公司
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