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Preparation method and application of myocardial metabolism PET imaging agent

A technology of nucleophilic substitution and acidic solvent, which is applied in the field of preparation of 18F-labeled myocardial metabolism PET imaging agent to achieve the effects of improving radiochemical purity and stability, improving reaction efficiency and optimizing preparation process

Pending Publication Date: 2022-07-12
BEIJING SINOTAU INT PHARMA TECH CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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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

[0084] 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

[0139] Example 1 Preparation of Compound I

[0140] 1) 18 Preparation of F ion solution

[0141] 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.

[0142] 2) 18 F ion enrichment

[0143] 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.

[0144] 3) 18 F ion elution

[0145] 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 0.5mL acetonitrile) with K 2 CO 3 4mg (dissolved in 0.1mL of water) was mixed to prepare a mixed solu...

Embodiment 2

[0162] The difference between Example 2 and Example 1 is only: 18 In the nucleophilic substitution reaction of F ions, the amount of compound I tert-butyl ester precursor is 3 mg, and the amount of compound I tert-butyl ester precursor (mg) / 18 The initial activity (Ci) of F was 3 mg / 4Ci (ie, 0.75:1), and other conditions were the same.

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Abstract

The invention provides a preparation method and application of a myocardial metabolism PET imaging agent trans-2-(2-(5-(fluorine [18F]) tridecyl) cyclopropyl) acetic acid (a compound I for short). Comprising the following steps: a nucleophilic substitution reaction: mixing activated < 18 > F ions with a solution containing a compound I tert-butyl ester precursor, and carrying out the nucleophilic substitution reaction to obtain an intermediate product solution containing the compound I tert-butyl ester; and a tert-butyl ester group removal reaction: adding an acidic solvent into the intermediate product solution of the tert-butyl ester of the compound I, and carrying out the tert-butyl ester group removal reaction to obtain a product containing the compound I. The yield and the labeling rate are improved, and the radiochemical purity is high.

Description

technical field [0001] The application 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 ...

Claims

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Application Information

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IPC IPC(8): C07C51/09C07C53/23C07C67/307C07C69/635C07B59/00A61K51/04A61K101/02
CPCC07C51/09C07C67/307C07B59/001A61K51/0402C07B2200/05C07C2601/02C07C69/635C07C53/23
Inventor 王跃张颖张爱丽徐新盛
Owner BEIJING SINOTAU INT PHARMA TECH CO LTD
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