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Preparation method and application of myocardial metabolism PET imaging agent

A technology of nucleophilic substitution and compound is applied in the field of preparation of 18F-labeled myocardial metabolism PET imaging agent, and achieves the effect of improving yield, improving labeling rate, and meeting the needs of automation

Active Publication Date: 2022-07-22
BEIJING SINOTAU INT PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However 18 There are still some limitations in the clinical application of F-FDG in brain tumor imaging with glucose metabolism as energy substrate, differential diagnosis of tumor and inflammation, etc.

Method used

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  • Preparation method and application of myocardial metabolism PET imaging agent
  • Preparation method and application of myocardial metabolism PET imaging agent
  • Preparation method and application of myocardial metabolism PET imaging agent

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preparation example Construction

[0083] 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 ...

Embodiment 1

[0153] Example 1 Preparation of compound I

[0154] 1) 18 Preparation of F ion solution

[0155] 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 solution of F ions, 18 F initial activity 4Ci.

[0156] 2) 18 F ion enrichment

[0157] 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 first used 5mL 0.5mol / L K 2 CO 3 Rinse, then rinse with 10mL water, after activation, 18 F ions are enriched on the QMA cartridge.

[0158] 3) 18 F ion elution

[0159] Elution with cave ether and alkali metal salt catalyst solution, elution 18 F ions into the reaction flask, specifically, the K 222 8mg (dissolved in 0.3mL acetonitrile) with K 2 CO 3 4mg (dissolved in 0.3mL water) was mixed to prepare a mixed solut...

Embodiment 2

[0175] The difference between Example 2 and Example 1 is: the amount of compound I tert-butyl ester precursor is 6 mg, and the amount of compound I tert-butyl ester precursor (mg) / 18 The initial activity (Ci) of F was 6mg / 4Ci (ie 1.5:1) and the rest of the conditions were the same.

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Abstract

The invention provides a preparation method and application of a liquid composition of a myocardial metabolism PET imaging agent trans-2-(2-(5-fluorine [18F] tridecyl) cyclopropyl) acetic acid (compound I for short), and the preparation method comprises the following steps: purifying a crude product containing the compound I by high performance liquid chromatography; wherein a mobile phase used in the high performance liquid chromatography purification step comprises ethanol and water. According to the present invention, the experiment process scheme is optimized, the use amount of the compound I tert-butyl ester precursor is changed, the reaction time for achieving the same labeling rate is shortened, the radioactivity of the initial 18F ion is improved, the labeling rate is improved, and the yield is improved.

Description

technical field [0001] The invention belongs to the technical field of chemical pharmacy, in particular to a kind of 18 Preparation method and application of F-labeled myocardial metabolism PET imaging agent. Background technique [0002] As the most advanced imaging technology in the field of biomedical engineering today, molecular medical imaging technology is the application of imaging methods to carry out qualitative and quantitative research at the cellular and molecular levels of biological processes in vivo, and to analyze biological physiology and pathology at the molecular level. Changes in real-time, dynamic, in vivo, non-invasive imaging technology. It is the key and core technology for the study of targeting, specific molecular probes and therapeutic drugs. Multimodal molecular imaging technology can realize the complementary advantages of different imaging equipment, so that the obtained imaging results are more accurate and reliable. Clinical practice has pr...

Claims

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Application Information

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IPC IPC(8): C07C51/09C07C51/47C07C53/23C07C67/307C07C69/635C07B59/00A61K51/04A61K101/02
CPCC07C51/09C07C51/47C07C67/307C07B59/001A61K51/0404C07B2200/05C07C2601/02C07C69/635C07C53/23
Inventor 王跃张颖张爱丽徐新盛
Owner BEIJING SINOTAU INT PHARMA TECH CO LTD
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