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Pyridazinone compound marked by fluorine-18, preparation method and applications

A technology for pyridazinones and compounds, which is applied in the field of fluorine-18 labeled pyridazinones and their preparation, can solve the problems of clinical application limitations, short half-life of imaging agents, etc., and achieve initial uptake value and high target-to-non-target ratio , good biological properties and high radiochemical purity

Inactive Publication Date: 2009-10-14
BEIJING NORMAL UNIVERSITY +1
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Problems solved by technology

However, the half-life of the above-mentioned imaging agents is short, and the clinical application is still greatly limited.

Method used

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  • Pyridazinone compound marked by fluorine-18, preparation method and applications
  • Pyridazinone compound marked by fluorine-18, preparation method and applications
  • Pyridazinone compound marked by fluorine-18, preparation method and applications

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Embodiment Construction

[0038]Taking n=2 as an example below, the present invention is described in detail through examples: a class of fluorine-18 labeled pyridazinone compounds:

[0039] (1) Synthesis of ligand OTs-P2OP:

[0040] a. Synthesis of furochloric acid (DCA)

[0041] Under ice bath, add 480mL of concentrated hydrochloric acid into a 1L four-neck flask. At 0-10°C, add 80g MnO in batches 2 , stirred, and slowly added dropwise 24g furfural. After stirring at room temperature for 30 min, the temperature was slowly raised to 60°C. At 60~80℃, add 42g MnO in batches 2 , heated up to 100°C. After the reaction until the liquid turned into an orange transparent solution, the reaction was continued for 30 min, cooled, and suction filtered. The precipitate was dissolved with 40 mL of ether and filtered. The filtrate was evaporated to remove the solvent, and recrystallized with 40 mL of water to obtain 31 g of furochloric acid as light pink flaky crystals. NMR spectrum: ( 1 HNMR, CDCl 3 )δ: ...

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Abstract

The invention discloses a pyridazinone compound marked by fluorine-18 with a molecular formula of FFPnOP and a preparation method and applications; in the formula, n is equal to 1, 2 or 3. By technical synthesis to ligand OTs-PnOP, the pyridazinone compound FFPnOP marked by radioactive fluorine-18 and stable reference compound FFPnOP are obtained by synthesis, wherein the stable reference compound is used for confirming the structure of the compound with radioactive marks; the compound has high radiochemical purity, good biological properties, high initial uptake value, simple preparation and low use cost, and is applied in the technical fields of radioactive drug chemistry and clinical nuclear medicine as a novel myocardial perfusion imaging agent marked by fluorine-18.

Description

Technical field [0001] The invention relates to the technical fields of fluorine-18 labeled radiopharmaceutical chemistry and clinical nuclear medicine, in particular to a class of fluorine-18 labeled pyridazinone compounds, their preparation method and application. Background technique [0002] Coronary heart disease is one of the most serious diseases threatening human health. In my country, the morbidity and mortality of coronary heart disease are on the rise. In 2007, the data released by the Ministry of Health showed that about 3 million people died of cardiovascular disease in my country every year, which has become the first cause of death among urban and rural people in my country, accounting for nearly 40% of the causes of death in my country. [0003] The use of myocardial perfusion imaging in non-invasive heart disease examinations began in the 1970s, and its great diagnostic value has been widely accepted around the world. It has become one of the most important...

Claims

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Application Information

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IPC IPC(8): C07D237/16A61K51/04A61K101/02
Inventor 张现忠牟甜甜杨文江景慧慧陆洁唐志刚张俊波王学斌
Owner BEIJING NORMAL UNIVERSITY
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