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Method for preparing 18F-FET

A 18F-FET, volume concentration technology, applied in chemical instruments and methods, cyanide reaction preparation, organic compound preparation, etc., can solve the problems of low efficiency, low chemical purity, long synthesis time, etc., to reduce waste The production amount, the improvement of chemical purity, and the effect of improving synthesis efficiency

Inactive Publication Date: 2012-02-01
GENERAL HOSPITAL OF PLA +1
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

The synthesis is carried out on the fluorine multifunctional module. Due to the complicated operation, it is difficult to promote, and a single mobile phase is used. After the product is separated, the chemical purity is not high, the synthesis time is long (50min), and the efficiency is not high (20%).

Method used

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  • Method for preparing 18F-FET
  • Method for preparing 18F-FET
  • Method for preparing 18F-FET

Examples

Experimental program
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Effect test

Embodiment 1

[0023] in the attached figure 1 The 18F-FET is synthesized on the common FDG module shown, and the radioactive F-18 ions produced by the accelerator are passed to the QMA column of the FDG module through nitrogen gas, K2.2.2 / K2CO 3 Acetonitrile aqueous solution (bottle A) pour F-18 from the QMA column into the reaction tube, remove acetonitrile under heating and open conditions, add 2 mL of acetonitrile (bottle B) to the reaction tube again, and remove acetonitrile. Add 0.6 mL of DMSO solution containing 10 mg of ethylene glycol p-toluenesulfonate (bottle C) into the reaction tube, heat to 85 ° C for 5 min, and add 0.6 mL of DMSO containing 9 mg of sodium tyrosine / 40 μL of 10% KOH to the reaction tube solution (bottle D), heat the reaction tube to 120°C for 5 minutes. Add 3 mL of 8% ethanol in water to the reaction tube, pass the mixed solution to a semi-prepared HPLC column for separation, the separation column is a C-18 column, and the mobile phase is an aqueous solution of...

Embodiment 2

[0025] in the attached figure 1 18F-FET is synthesized on the common FDG module shown, but the semi-preparative HPLC mobile phase is changed to improve the chemical purity of the product: the radioactive F-18 ion produced by the accelerator is passed to the QMA column of the FDG module through nitrogen, K2.2.2 / K2CO 3 Acetonitrile aqueous solution (bottle A) pour F-18 from the QMA column into the reaction tube, remove acetonitrile under heating and open conditions, add 2 mL of acetonitrile (bottle B) to the reaction tube again, and remove acetonitrile. Add 0.6 mL of acetonitrile solution containing 10 mg of ethylene glycol p-toluenesulfonate (bottle C) into the reaction tube, heat to 85 ° C for 5 minutes, blow nitrogen to remove acetonitrile to 0.1 mL, add 0.6 mL of 9 mg of tyrosine to the reaction tube NaCl / 40 μL 10% KOH in DMSO solution (bottle D), heat the reaction tube to 120°C for 4 minutes, mix with nitrogen gas, and then heat for 1 minute. Add 3mL of 8% ethanol in wat...

Embodiment 3

[0027] in the attached figure 1 The 18F-FET is synthesized on the common FDG module shown, and the radioactive F-18 ions produced by the accelerator are passed to the QMA column of the FDG module through nitrogen gas, K2.2.2 / K2CO 3Acetonitrile aqueous solution (bottle A) pour F-18 from the QMA column into the reaction tube, remove acetonitrile under heating and open conditions, add 2 mL of acetonitrile (bottle B) to the reaction tube again, and remove acetonitrile. Add 0.6 mL of acetonitrile solution containing 10 mg of ethylene glycol p-toluenesulfonate (bottle C) into the reaction tube, heat to 85 ° C for 5 min, and directly add 0.6 mL of 9 mg sodium tyrosine / 40 μL of 10% KOH to the reaction tube DMSO (bottle D), heat the reaction tube to 120°C for 5 min. Add 3 mL of 8% ethanol in water to the reaction tube, pass the mixed solution to a semi-prepared HPLC column for separation, the separation column is a C-18 column, and the mobile phase is an aqueous solution of 6% ethanol...

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Abstract

The invention relates to a method for automatically synthesizing and purifying O-(2-18F-fluoroethyl)-L-tyrosine (18F-FET). Ethylene glycol p-toluenesulfonate is used as a raw material and reacted with 18F-nucleophile on a fluorodeoxyglucose (FDG) module, the reaction product is not purified and is reacted with L-tyrosine salt in the same reactor, the product is purified by different mobile phases of high performance liquid chromatography (HPLC), and the separated product is neutralized and then filtered by a sterile filtration membrane to meet the injection requirement. The process can be automatically operated on the common FDG module, and has the advantages of short synthesis time (30 minutes, comprising HPLC purification) and high yield (40 percent, correction).

Description

technical field [0001] The invention relates to an automatic synthesis method of radiopharmaceuticals for positron tomography (PET) diagnosis, in particular to a synthesis method using tyrosine as a precursor under heating conditions 18 F-FET (O-(2-18F-fluoroethyl)-L-tyrosine) method. Background technique [0002] O-(2-18F-fluoroethyl)-L-tyrosine ( 18 F-FET) is an F-18-labeled amino acid that can be synthesized in large quantities and can be supplied clinically in the form of a distribution center. It has been used in the grading and prognosis of glioma, the assessment of the range of glioma, and the identification of tumor recurrence Necrosis with radiotherapy, evaluation of the efficacy of various tumor treatments, etc., and achieved satisfactory results. [0003] 18 The synthesis method of F-FET has been reported at home and abroad. "Synthesis and radiopharmacology of O-(2-[18F]fluoroethyl-L-Tyrosine for tumor imaging" (Wester H, et al, J Nucl Med, 1999, 40: 205-212),...

Claims

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Application Information

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IPC IPC(8): C07C229/36C07C227/16
Inventor 张锦明黄伟田嘉禾张晓军
Owner GENERAL HOSPITAL OF PLA
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