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Novel 18f-labeled substituted quinazoline compounds and their preparation methods and tumor pet imaging applications

A technology of quinazolines and 18F, which is applied in the field of new 18F-labeled substituted quinazolines to achieve high labeling rate, short labeling time, and high tumor uptake

Inactive Publication Date: 2016-02-17
BEIJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, the studies on labeled quinazoline derivatives are mainly focused on their application as EGFR inhibitors for imaging, and most of these studies have achieved good results, while the research on labeled quinazoline derivatives as JAK3 inhibitors There are few reports at home and abroad on the study of

Method used

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  • Novel 18f-labeled substituted quinazoline compounds and their preparation methods and tumor pet imaging applications
  • Novel 18f-labeled substituted quinazoline compounds and their preparation methods and tumor pet imaging applications
  • Novel 18f-labeled substituted quinazoline compounds and their preparation methods and tumor pet imaging applications

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Experimental program
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Embodiment

[0066] Embodiment formula G: in formula A, R1 is in para-position, R2=methoxyl group ([ 18 F]-FEWHIP131)

[0067]

[0068] One, prepared according to the following steps is that R1 is in the para-position in formula A, and the compound of R2=methoxyl group ([ 18 F]-FEWHIP131), including the synthesis of its labeling precursor (R1' is in the para position in formula B, R2 = methoxy) and the synthesis of the labeling precursor 19 Synthesis of F Substitutes and Radiochemical Synthesis in Three Parts

[0069] 1. Synthesis of labeled precursors

[0070] According to the following steps, the compound in which R1" is in the para position and R2 = methoxy group in formula C is prepared according to the following steps

[0071] 1.13, Synthesis of ethyl 4-dimethoxybenzoate

[0072] 3,4-Dimethoxybenzoic acid (10g, 0.055mol) and ethanol (100mL) were added into a 250mL reaction flask, and concentrated H2SO4 (8mL) was added dropwise under stirring, heated to reflux, followed by TLC m...

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Abstract

The invention provides a novel <18>F marked substituted quinazoline compound. The novel <18>F marked substituted quinazoline compound is characterized in that one end of the novel <18>F marked substituted quinazoline compound has a <18>F substituted alkyloxy structure; the other end of the compound has a 6,7-substituted quinazoline structure, and a substituent R1 is positioned in the 4 position of a quinazoline maternal, and is a 2-, 3-, 4-<18>F substituted alkyloxy group; and a substituent R2 is positioned in the 6 position of the quinazoline maternal, and is a methoxyethoxy group, a methoxy group, or a morpholinepropanolato group. The structural formula of the compound is shown as A in the specification. Results of experiments show that the compound has the advantages of good bioactivity, good serum stability, low intake in tissues of the liver and the like, and high enrichment and slow removal rate in tumors, and the marking precursor of the compound has the advantages of easy synthesis, extremely high marking rate and the like, so the compound has a huge potential for the tumor PET development.

Description

Technical field: [0001] The present invention relates to a new class of 18 The F-labeled substituted quinazoline compound, its preparation method and its application as a tumor positron emission tomography (PET) molecular probe. Background technique: [0002] Positron emission tomography (PET) is a powerful molecular imaging technique that is rapidly developing to study biological 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. [0003] 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 its hydrogen-like properties will not cause significant changes in the spatial structure of the labeled molecules. Therefore, yes 18 The study of F-labeled PET imaging agents has...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D239/94A61K51/04A61K101/02
Inventor 齐传民李石磊王潇何勇许荆立冯曼陈玉蓉
Owner BEIJING NORMAL UNIVERSITY
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