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Fluoro labelled aliphatic acid myocardial metabolic imaging agent 14 (R,S)-Fluoro[18F]-6-thio cydonic acid purifying method

A technology of thioheptadecanoic acid and myocardial metabolism, which is applied in the field of fluorine-labeled fatty acid myocardial metabolism imaging agent, which can solve problems such as inability to work deeply.

Inactive Publication Date: 2004-09-15
JIANGSU INST OF NUCLEAR MEDICINE
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Problems solved by technology

In foreign countries, the work of SPECT metabolic imaging of fatty acid myocardium has been very in-depth. 123 I, the job cannot go deep

Method used

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  • Fluoro labelled aliphatic acid myocardial metabolic imaging agent 14 (R,S)-Fluoro[18F]-6-thio cydonic acid purifying method
  • Fluoro labelled aliphatic acid myocardial metabolic imaging agent 14 (R,S)-Fluoro[18F]-6-thio cydonic acid purifying method
  • Fluoro labelled aliphatic acid myocardial metabolic imaging agent 14 (R,S)-Fluoro[18F]-6-thio cydonic acid purifying method

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Embodiment Construction

[0019] 1, 18 F mark

[0020]

[0021] Depend on 18 O(p,n) 18 Carrier-free generated by F reaction 18 f - (740~1850MBq), enriched on the anion exchange column QMA, with 1ml K 2 CO 3 -K 2.2.2 The solution was rinsed into a reaction tube, heated and blown dry in an oil bath at 105° C. under nitrogen flow, and the residue was evaporated to dryness azeotropically with anhydrous acetonitrile (3×1 ml). Add 14(R,S)-toluenesulfonyl-6-thio-heptadecanoic acid benzyl ester (3-10mg) in acetonitrile solution (1ml), and react in an oil bath at 90-95°C for 20min. Add potassium hydroxide (0.2mol / L, 0.5ml) to the above reaction tube, and continue the ester hydrolysis reaction in an oil bath at 90-95°C. After reacting for 5 minutes, a) immediately add acetic acid (50μl) and water (1ml) , pour off the aqueous solution, and use ethanol (0.5 ~ 1ml) to remove the adsorbed on the wall of the reaction tube 18 F-FTHA was dissolved and transferred to a clean penicillin bottle; b) the reactio...

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Abstract

The invention is a method to purify a fluorin-labeled fatty acid cardiac muscle metabolism developer 14(R, S)-fluoro[18F]-6-thio-daturic acid, relating to a radioactive positron drug synthesis. By reference to documents, it uses 8-bromo-1-capryl alcohol as raw material, gradually synthesizes to obtain label precursor 14(R,S)-(p-toluenesulfonyl)-6-thio- benzyl margarate FTHA-OTs and nonradioactive FTHA, and make nucleophilic fluorin labeling on the label precursor to make 18F-FTHA. It improves the method to purify resultant through nucleophilic fluorin labeling, and the reacting mixture is prepared not by HPLC separation, but by adding in distilled water while hot after the ester hydrolyzes, or by Sep-Pak18C column separation. The radioactive chemical output and purity of 18F-FTHA are somewhat heightened, and the detection shows that FTHA and 18F-FTHA have consistent retention time.

Description

technical field [0001] A fatty acid metabolism imaging agent 14(R,S)-fluoro[ 18 The purification method of F]-6-thioheptadecanoic acid relates to a fluorine-labeled fatty acid myocardial metabolism imaging agent. Background technique [0002] In the past ten years, positron emission tomography (PET) imaging has been widely used clinically in the clinical and basic research of tumors, neuropsychiatric diseases and cardiovascular diseases, and has gradually become a new scientific research method for gene function and new drug development research. . The application and development of PET are inseparable from PET positron radiopharmaceuticals. Positron radiopharmaceuticals commonly used in clinical practice cannot be imported from abroad due to their short half-life, but must be developed by themselves. Among medical short half-life nuclides, 18 F has a relatively long half-life (110min), and can be used at close range outside PET centers. 18 The research of various positr...

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Application Information

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IPC IPC(8): A61K51/00C07C319/28C07C323/51
Inventor 吴春英陆春雄纪书仁林祥通张政伟陈正平蒋泉福傅榕赓张同兴李晓敏王颂佩朱钧清曹国宪项景德薛方平管一晖赵军刘兴党刘平
Owner JIANGSU INST OF NUCLEAR MEDICINE
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