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Novel 18F labeled p-nitro benzoyl amino acid compound and preparation method and application thereof

A technology of nitrobenzoylamino acid and nitrobenzoyl structure is applied in the field of novel 18F-labeled p-nitrobenzoyl amino acid compounds, and achieves the effects of simple synthesis, good specificity and short total labeling time

Inactive Publication Date: 2010-06-09
BEIJING NORMAL UNIVERSITY
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  • Abstract
  • Description
  • Claims
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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 compound and preparation method and application thereof
  • Novel 18F labeled p-nitro benzoyl amino acid compound and preparation method and application thereof
  • Novel 18F labeled p-nitro benzoyl amino acid compound and preparation method and application thereof

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Embodiment

[0075] Prepared according to the following steps is the compound whose R group is isopropyl in formula A, including the synthesis of the labeling precursor (the compound in which R is isopropyl in formula B) and the synthesis of the precursor compound 18 F labels, hydrolyzes two fractions.

[0076] 1) Synthesis of the labeled precursor (the compound in which R is an isopropyl group in formula B)

[0077] 1.12, the synthesis of 4-dinitrobenzoic acid (formula H)

[0078] 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, rinse 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 while it is hot, and use Wash with a small amount of water,...

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Abstract

The invention designs an 18F labeled p-nitro benzoyl amino acid compound, which is characterized by simultaneously having 2-18F-4-nitro-benzoyl structure and an alpha-amino acid structure, and a substituent R positioned on a carboxyl alpha position, wherein the substituent R comprises hydrogen, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, benzyl, 2-methylthio-ethyl, carboxyethyl, carboxy-propyl, phenyl and imidazole methyl. Two end structures are directly connected with each other through an amido bond. The compound has a structure formula A. The compound can be synthesized simply and has a high labeling rate. The compound is absorbed for a large amount in tumor tissues and is eliminated slowly, but in normal tissues and blood, the compound is absorbed for a small amount or is eliminated quickly. The compound has a very high tumor / blood specific value and a very high tumor / normal tissue specific value, in particular a very high brain normal tissue specific value, and has a high discrimination degree of tumor and brain background. The invention also relates to the application of the compound as a PET brain tumor imaging agent.

Description

Technical field: [0001] The present invention relates to a new class of 18 F-labeled p-nitrobenzoyl amino acid compound, its chemical preparation method and its application as a tumor (especially brain 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 al...

Claims

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Application Information

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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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