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18F-labeled isoquinolinopyridazinone compound as well as synthesis method and application thereof

A synthesis method and technology of isoquinoline, which are applied in the directions of organic chemistry methods, chemical instruments and methods, isotope introduction of heterocyclic compounds, etc., can solve problems such as application to be studied, and achieve the effect of high stability

Inactive Publication Date: 2020-06-26
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In summary, a 18 F-labeled isoquinolinopyridazinone compounds and their synthesis methods and applications are yet to be studied

Method used

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  • 18F-labeled isoquinolinopyridazinone compound as well as synthesis method and application thereof
  • 18F-labeled isoquinolinopyridazinone compound as well as synthesis method and application thereof
  • 18F-labeled isoquinolinopyridazinone compound as well as synthesis method and application thereof

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Embodiment Construction

[0033] In order to further illustrate the technical effect of the present invention, the present invention is specifically described below through examples.

[0034] 18 The specific preparation method of the isoquinolinopyridazinone compound of F label is as follows:

[0035]

[0036] Compound 1N-Boc-4-piperidone (10g, 50mmol) was dissolved in 80ml of anhydrous toluene, added p-toluenesulfonic acid monohydrate (0.3g, 1.5mmol) and tetrahydropyrrole (4.3g, 60mmol), heated Reflux reaction, the water produced by the reaction was separated with an oil-water separator, cooled to room temperature after 3h, added p-toluenesulfonic acid monohydrate (0.3g, 1.5mmol) and ethyl glyoxylate (50% toluene solution) (11ml , 55mmol), heated to reflux for 2h, cooled to room temperature, concentrated the reaction solution to about 20ml, slowly added 4M hydrochloric acid (54ml) dropwise under vigorous stirring, and continued to stir overnight at room temperature. The organic phase was separate...

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Abstract

The invention discloses an 18F-labeled isoquinolinopyridazinone compound as well as a synthesis method and application thereof and belongs to the field of imaging agents. According to the invention, isoquinolinopyridazinone compounds are spliced and optimized through a pharmaceutical chemistry principle, brand-new organic small molecules targeting myocardial mitochondrial membranes are prepared onthe basis of not changing the structure of active groups of key drug effects, and 18F radioactive isotopes are labeled through a positron nuclide labeling experiment; the 18F-labeled isoquinolinopyridazinone compound prepared by the invention has relatively good myocardial targeting and is a myocardial imaging agent with an excellent effect.

Description

technical field [0001] The invention belongs to the field of imaging agents, in particular to 18 F-labeled isoquinolinopyridazinone compounds and their synthesis methods and applications. Background technique [0002] Cardiovascular diseases (CVDs) are the leading cause of death in the world today, according to the World Health Organization, American Heart Association, and National Center for Cardiovascular Diseases. Nuclear cardiology SPECT and PET stress myocardial perfusion imaging have been fully affirmed by the relevant guidelines of the American College of Cardiology / American Heart Association / American Society of Nuclear Cardiology (ACC / AHA / ASNC), and risk stratification of CAD patients can It can predict the probability of sudden cardiac death or non-fatal myocardial infarction, reduce the occurrence of malignant cardiac events, and select appropriate patients for revascularization or drug treatment. The radionuclide myocardial imaging currently used clinically is m...

Claims

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Application Information

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IPC IPC(8): C07D455/03C07D471/14C07B59/00A61K51/04A61K101/02
CPCA61K51/0459C07B59/002C07B2200/05C07D455/03C07D471/14
Inventor 吴小艾范成中潘立立
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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