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Liquid composition of compound I as well as preparation method and application of liquid composition

A technology for liquid compositions and compounds, applied in organic chemistry methods, chemical instruments and methods, introduction of isotopes into organic compounds, etc., can solve the problems of clinical application limitations, short half-life of imaging agents, etc., and improve radiochemical purity and stability. , the effect of improving radioactivity and ensuring stability

Active Publication Date: 2022-08-02
BEIJING SINOTAU INT PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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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  • Liquid composition of compound I as well as preparation method and application of liquid composition
  • Liquid composition of compound I as well as preparation method and application of liquid composition
  • Liquid composition of compound I as well as preparation method and application of liquid composition

Examples

Experimental program
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Effect test

preparation example Construction

[0114] In the prior art, amino polyether (K 222) is the high dilution method proposed by Lehn et al., which is one of the typical non-template ion synthesis methods. The specific steps are: 8-Diacyl chloride-3,6-dioxoctane was dissolved in a large amount of benzene solvent, and heated for 8 hours, then reduced by tetrahydroaluminum lithium for 24 hours, and then separated and recrystallized by column chromatography to obtain amino polyether (K 222 ). The method requires a large amount of solvent, such as benzene, the synthesis route is long, the operation is complicated, the yield is low, and the economic benefit is not high. In addition to the high dilution method, aminopolyether (K 222 ) is another classical synthesis method proposed by Kulstad and Malmsten using Na 2 CO 3 Equal to template in acetonitrile to obtain aminopolyether (K 222 ) sodium iodide complex, and then decomplexed by resin to obtain aminopolyether (K 222 ) synthesis method. The specific steps are a...

Embodiment 1

[0214] Example 1 Preparation of Compound I

[0215] 1) 18 Preparation of F ion solution

[0216] oxygenated [ 18 The water 2g of O] is transported to the accelerator target, and the accelerator is activated to generate a proton beam to bombard the oxygen-containing [ 18 O] water, producing a 18 The solution of F ions, this example uses a large dose to start 18 F, 18 The F initial activity is 3.5Ci.

[0217] 2) 18 F ion enrichment

[0218] prepared above 18 The solution of F ions is passed through an anion exchange solid phase extraction cartridge (Waters brand QMA cartridge, the QMA cartridge is preferably 1 mol / L NaHCO 3 activation), 18 F ions are enriched on the QMA cartridge.

[0219] 3) 18 F ion elution

[0220] Elution with cave ether and alkali metal salt catalyst solution, elution 18 F ions into the reaction flask, specifically, the K 222 15mg (dissolved in 0.9mL acetonitrile) with K 2 CO 3 1.5 mg (dissolved in 0.1 mL of water) was mixed to prepare a m...

Embodiment 2

[0234] The difference between Example 2 and Example 1 is only: 5) 8 In the nucleophilic substitution reaction of F ions, the amount of compound I precursor was 20 mg.

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Abstract

The invention provides a compound I liquid composition, a preparation method and application thereof, and the compound I liquid composition is selected from one or more than two of vitamin C, vitamin C sodium and gentisic acid. By optimizing process parameters and the process flow, the method can be suitable for mass production, and the obtained product is high in radiochemical purity, high in activity concentration, good in product stability and high and stable in yield or yield.

Description

technical field [0001] The application belongs to the technical field of chemical pharmacy, and particularly relates to a liquid composition of compound I, a preparation method and uses thereof. Background technique [0002] Coronary heart disease is one of the most serious diseases that threaten human health. In my country, both 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 every year in my country, which has become the first cause of death in my country's urban and rural populations, accounting for nearly 40% of the causes of death in my country. [0003] The use of myocardial perfusion imaging for non-invasive examination of heart disease began in the 1970s. Its huge diagnostic value has been widely accepted around the world, and it has become one of the most important imaging methods for coronary heart disease diagnosis, efficac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/04A61K51/12C07D403/12C07B59/00A61K101/02
CPCA61K51/0459A61K51/121C07D403/12C07B59/002C07B2200/05
Inventor 王跃张颖张爱丽徐新盛
Owner BEIJING SINOTAU INT PHARMA TECH CO LTD
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