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Novel 18F labeled p-nitro benzoyl amino acid derivatives, preparation method and application thereof in tumor imaging

A technology of nitrobenzoyl amino acid and labeling method, which is applied in the field of novel 18F-labeled p-nitrobenzoyl amino acid derivatives, preparation and application in tumor imaging, achieving less radioactive loss, simple synthesis, and raw materials Inexpensive and easy to get effects

Inactive Publication Date: 2010-06-09
BEIJING NORMAL UNIVERSITY
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Problems solved by technology

In addition, although some labeled amino acid derivatives do not participate in protein synthesis, they can also be used as imaging agents as long as they can be transported by the transport system of tumor tissue. Therefore, certain amino acid derivatives labeled with radionuclides Drugs may also be tumor imaging agents

Method used

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  • Novel 18F labeled p-nitro benzoyl amino acid derivatives, preparation method and application thereof in tumor imaging
  • Novel 18F labeled p-nitro benzoyl amino acid derivatives, preparation method and application thereof in tumor imaging
  • Novel 18F labeled p-nitro benzoyl amino acid derivatives, preparation method and application thereof in tumor imaging

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Embodiment

[0080] Prepared according to the following steps is R in formula A 1 The group is isopropyl, R 2 The compound whose radical is a methoxyl group includes a labeling precursor (R in formula B 1 The group is isopropyl, R 2 The synthesis of compounds whose group is methoxy) and the synthesis of precursor compounds 18 F marks two parts.

[0081] 1) labeled precursor (R in formula B 1 The group is isopropyl, R 2 Synthesis of compounds whose group is methoxy)

[0082] 1.1 Synthesis of 2,4-dinitrobenzoic acid (formula J)

[0083] In a three-necked flask, add 5.5 grams (0.03 mol) of 2,4-dinitrotoluene to 30 mL of pyridine and 50 mL of water, heat, and maintain the temperature at 78-83 ° C, and add 32 g of potassium permanganate in batches ( 0.202mol), after adding in 6-8h, wash the potassium permanganate sticking to the inner wall of the condenser tube end with 10mL of water into the bottle, continue to react for 3h, until the potassium permanganate is completely faded, filter w...

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Abstract

The invention designs novel 18F labeled p-nitro benzoyl amino acid derivatives. The derivatives are characterized in that one end of the derivatives is provided with 2-fluorine 18-4-nitro benzoyl structure, and the other end of the derivatives is provided with alpha-amino acid derivative structure (derived group R2 is methoxyl group, methylamino group and N,N-dimethylamino group respectively); and substituent R1 is positioned on an alpha site of carbonyl group and is hydrogen, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, benzyl group, 2-methylthio-ethyl group, carboxyethyl group, carboxypropyl group, phenyl or imidazole methyl group. The structures at two ends are directly connected through amido bond. The structure of the derivatives is shown in a formula A. The compounds are simple to synthesize, fast to label, large in the amount of initial absorption and slow to clear in tumor tissue, low in uptake or fast to clear in other normal tissue and blood and high in degree of distinguishing tumor from background. The invention also relates to the application of the compounds serving as a PET brain tumor imaging agent. R2=OMe, HNCH3.

Description

Technical field: [0001] The present invention relates to a new 18 F-labeled p-nitrobenzoyl amino acid derivatives, their chemical preparation method and their application as a tumor imaging agent for positron emission tomography (PET). Background technique: [0002] The early diagnosis of tumors is a hot topic in today's medicine, and positron emission tomography (PET) has received great attention as an increasingly popular means, so the breakthrough of early diagnosis of tumors depends on PET tumor imaging agents development. [0003] radionuclide 18 F is very suitable as an imaging nuclide for PET because of its excellent nuclide properties. [0004] The most widely used positron-emitting radiopharmaceuticals are 18 F-deoxyglucose ( 18 F-FDG), has been widely used in the research and clinical diagnosis of tumors, coronary heart disease and neuropsychiatric diseases. However, due to the large intake of FDG in normal brain tissue, there is also high FDG absorption in n...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C233/83C07C231/12A61K51/04A61K101/02
Inventor 齐传民乔雅丽刘航贺勇张淑婷李桂霞许荆立
Owner BEIJING NORMAL UNIVERSITY
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