Novel 18F labeled substituted benzimidazole compounds, preparation method thereof and PET tumor imaging application

Abstract

The invention provides novel 18F labeled substituted benzimidazole compounds, which are characterized in that: one end of each compound contains an 18F substituted alkoxy structure, and the other end contains a 6-carboxyl / H benzimidazole structure; a substituent group R1, located on the site 2 of benzimidazole matrix, is hydrogen, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, benzyl, 2-methylthio ethyl and phenyl; a substituent group R2, located on the site 4 of benzimidazole matrix, is hydrogen, methyl and ethyl; and the structure of the compound is shown in formula A, wherein n is between 1 and 5, R2 is H, Me and Et, X is COOH and H. Experiments show that the compounds have high bioactivity such as fast serum removal, high serum stability and relatively low intake in tissues or organs such as liver and relatively high enrichment and slow removal rate in tumor cells, and therefore the compounds have relatively high tumor / background value and are favorable for PET tumor imaging. Meanwhile, the labeled precursor of the compounds is easy to synthesize and the labeling rate is extremely high; and such advantages indicate that the compounds have the tremendous potential to become PET tumor imaging agents.

Description

Technical field: The present invention relates to a new class of 18 The F-labeled substituted benzimidazole compound, its preparation method and its application as a tumor positron emission tomography (PET) molecular probe. Background technique: Positron emission tomography (PET) is a powerful molecular imaging technique that is rapidly developing to study physiological processes such as substance metabolism, receptor binding, and biochemical mechanisms in living tissues. Today, PET has been widely used in the early diagnosis and postoperative evaluation of tumors, which has great research value and market demand. Among the nuclides commonly used in PET imaging, 18 F has a longer half-life (t 1 / 2 =110min), and has a lower radiation dose and a shorter range to the tissue, and at the same time, its hydrogen-like properties will not cause obvious changes in the spatial structure of the labeled molecules. Therefore, yes 18 The study of F-labeled PET imaging agents has beco...

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And related researches are rarely reported at home and abroad, which also makes this invention highly innovative and has good application prospects.

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