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Chemical synthesizer capable of preparing multiple fluoro-marking agent

A technology of chemical synthesis and reagents, applied in chemical instruments and methods, chemical/physical processes, radioactive preparations in vivo, etc., can solve problems such as high production costs, lack of chemical synthesis equipment, and inseparable steps

Inactive Publication Date: 2007-05-23
SHANGHAI RES INST OF CHEM IND +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, development of positron radiopharmaceuticals has been relatively slow, using 18 F-FDG imaging accounts for more than 90%, and other drugs are rarely used
[0005] The main reason restricting the research and development of positron radiopharmaceuticals is that the raw materials of oxygen-18 are expensive, resulting in high cost of new drug development and trial production, and the chemical synthesis equipment of positron radiopharmaceuticals is relatively lacking, and the existing synthesis systems are all dedicated to the synthesis of single drugs The chemical synthesis system can only synthesize a single positron radiopharmaceutical, its parameters are fixed, and each step is inseparable
Great inconvenience to the research and clinical application of new drugs
At the same time, many existing systems still have shortcomings such as long synthesis time, low yield, large consumption of oxygen-18 raw materials, and high production costs.

Method used

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  • Chemical synthesizer capable of preparing multiple fluoro-marking agent
  • Chemical synthesizer capable of preparing multiple fluoro-marking agent
  • Chemical synthesizer capable of preparing multiple fluoro-marking agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024]This device separates and purifies to obtain nucleophilic reaction 18 f - ion.

[0025] As shown in Figure 2, the preparation of separation and purification 18 f - Ions, a schematic diagram of the process structure for recovering oxygen-18 raw materials. First, prepare K with potassium carbonate 2.22 Anhydrous acetonitrile solution, it is added in the reagent bottle 22, anhydrous acetonitrile is added in the reagent bottle 23, open accelerator and carry out 18 O(p,n) 18 F reaction, then just can carry out preparation operation, concrete operation steps are as follows:

[0026] 1. Pass by the accelerator 18 O(p,n) 18 F reaction generation 18 F, on-target 18 F is transmitted by argon, through the three-way solenoid valve 12, 18 f - The ions are captured by the anion column QMA47, and the unreacted oxygen-18 raw material is purified after passing through the IC-H column 48 and IC-OH column 49 to remove the heavy metal ions from the metal target, and enters the o...

Embodiment 2

[0031] Prepared using this device 18 F-FDG.

[0032] As shown in Figure 3, the preparation 18 Schematic diagram of the flow structure of F-FDG. First, the K containing potassium carbonate 2.2.2 Add anhydrous acetonitrile solution to reagent bottle 22, add anhydrous acetonitrile to reagent bottle 23, add dilute alkali solution (0.3N NaOH or KOH) to reagent bottle 24, add dilute acid (1N HCl) to reagent bottle In 25, mannose trifluoride dissolved in anhydrous acetonitrile is added in the reagent bottle 26, pure water is added in the reagent bottle 27, and the accelerator is turned on to carry out 18 O(p,n) 18 F reaction, then just can carry out preparation operation, concrete operation steps are as follows:

[0033] 1. according to the step 1,2,3 of embodiment 1, will isolate and purify 18 f - Ions are transferred to the tubular reactor 37;

[0034] 2. Open the two-way solenoid valve 20, open the thermostat 45, adjust the temperature of the resistance wire 43 through the...

Embodiment 3

[0045] Prepared using this device 18 F-MPPF.

[0046] As shown in Figure 4, the preparation 18 Schematic diagram of the flow structure of F-MPPF. First, the K containing potassium carbonate 2.2.2 Add anhydrous acetonitrile solution to reagent bottle 22, add anhydrous acetonitrile to reagent bottle 23, add dilute alkali solution (0.3N NaOH or KOH) to reagent bottle 24, add dilute acid (1N HCl) to reagent bottle In 25, 4-(2'-methoxy-phenyl)-1-[2'-(n-2"-pyridyl)-p-nitrobenzamide]-ethylpiperazine (MPPNO 2 ) dissolved in anhydrous dimethyl sulfoxide (DMSO) was added to reagent bottle 28, anhydrous ether was added to reagent bottle 29, methanol / tetrahydrofuran (THF) mixed solution was added to reagent bottle 30, and HPLC washing liquid was added to In the reagent bottle 31, open the accelerator to carry out 18 O(p,n) 18 F reaction, then just can carry out preparation operation, concrete operation steps are as follows:

[0047] 1. according to the step 1,2,3 of embodiment 1, w...

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Abstract

The invention relates to a chemical synthesizer for preparing kinds of fluorine marking agent, wherein said device has dual-circle tubular reactor system; each circle has independent temperature control system and feeding system, to transmit material at positive or passive pressure, and process acid or alkali hydrolysis, and adjust the operation parameters via different drug parameters; and the invention has oxygen-18 recycle system when prepare 18F ion, to reduce the material consumption and cost. The invention can synthesize F-18 positron radioactive drug, to reduce the reaction time and improve the efficiency.

Description

technical field [0001] The invention relates to a device for preparing positron radiopharmaceuticals, in particular to a device capable of preparing various F-18 labeled positron radiopharmaceuticals. Background technique [0002] In nuclear medicine diagnostic applications, such as Positron Emission Computed Tomography (PET), positron radiopharmaceuticals must be used, usually labeled with elements with short half-lives, such as 18 F. 15 O. 13 N. 11 C et al. Since the physical half-life of the radionuclide fluorine-18 is 110 minutes, F-18-labeled positron radiopharmaceuticals are the most widely used. for example 18 F-FDG (2- 18 F-2 deoxy-β-D-glucose) can be widely used in the diagnosis of malignant tumors, the determination of glucose metabolism in the myocardium and brain, etc.; 18 F-MPPF (4- 18 F fluoro-N-2-[1-(2-methoxyphenyl)-1-piperazinylethyl]-N-2-pyridyl-benzamide), can be applied to such as depression, insomnia, anxiety diagnosis of nervous system diseases...

Claims

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Application Information

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IPC IPC(8): B01J19/00A61K51/00A61K101/02
Inventor 伍昭化刘平肖斌许震生周建耀张政伟秦川江姜永悦陈代传
Owner SHANGHAI RES INST OF CHEM IND
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