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Method for synthesizing <18>F ethyl choline

A technology of ethylcholine and dimethylethanolamine, which is applied in the direction of organic chemical methods, chemical instruments and methods, and the preparation of organic compounds, can solve the problems of lack of versatility, and achieve simple production equipment and processes and high reaction yields The effect of high and low production cost

Inactive Publication Date: 2017-09-08
SHENYANG INSTITUTE OF CHEMICAL TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Hara et al. automated the synthesis using specialized modules 18 F-FECH, with 18 Compared to F-FCH, 18 The synthesis yield of F-FECH is higher and more stable, which is convenient for clinical application, but the method lacks versatility

Method used

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  • Method for synthesizing &lt;18&gt;F ethyl choline

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] A 2-bromotrifluoromethanesulfonic acid ethyl ester (BrC 2 h 4 OTf) was synthesized as a starting material 18 F ethylcholine ( 18 F-FECH) method.

[0030] (1) Continuous bombardment of H with a cyclotron proton beam 2 18 O, production 18 f - , with helium 18 f - Transfer from the target to the target water recovery bottle of the synthesis module.

[0031] (2) Press out from the target water recovery bottle 18 f － Through the QMA column, 18 f － Captured on the QMA column.

[0032] (3) with 0.9ml K 2.2.2 / K 2 CO 3 The solution will be adsorbed on the QMA column 18 f － Rinse to the reaction tube, and then start heating the reaction tube to remove the water and acetonitrile in the system. After evaporating to dryness, continue to add 0.5 ml of anhydrous acetonitrile to the reaction flask, and heat and evaporate to dryness again.

[0033] (4) Add BrC dissolved in o-dichlorobenzene 2 h 4 OTf (10 μl BrC 2 h 4 OTf is dissolved in 1.0ml o-dichlorobenzene...

Embodiment 2

[0037] A 2-bromotrifluoromethanesulfonic acid ethyl ester (BrC 2 h 4 OTf) was synthesized as a starting material 18 F ethylcholine ( 18 F-FECH) method.

[0038] (1) Continuous bombardment of H with a cyclotron proton beam 2 18 O, production 18 f - , with helium 18 f - Transfer from the target to the target water recovery bottle of the synthesis module.

[0039] (2) Press out from the target water recovery bottle 18 f － Through the QMA column, 18 f － Captured on the QMA column.

[0040] (3) with 0.9ml K 2.2.2 / K 2 CO 3 The solution will be adsorbed on the QMA column 18 f － Rinse to the reaction tube, and then start heating the reaction tube to remove the water and acetonitrile in the system. After evaporating to dryness, continue to add 0.5 ml of anhydrous acetonitrile to the reaction flask, and heat and evaporate to dryness again.

[0041] (4) Add BrC dissolved in o-dichlorobenzene 2 h 4 OTf (15 μl BrC 2 h 4 OTf is dissolved in 1.0ml o-dichlorobenzene...

Embodiment 3

[0045] A 2-bromotrifluoromethanesulfonic acid ethyl ester (BrC 2 h 4 OTf) was synthesized as a starting material 18 F ethylcholine ( 18 F-FECH) method.

[0046] (1) Continuous bombardment of H with a cyclotron proton beam 2 18 O, production 18 f - , with helium 18 f - Transfer from the target to the target water recovery bottle of the synthesis module.

[0047] (2) Press out from the target water recovery bottle 18 f － Through the QMA column, 18 f － Captured on the QMA column.

[0048] (3) with 0.9ml K 2.2.2 / K 2 CO 3 The solution will be adsorbed on the QMA column 18 f － Rinse to the reaction tube, and then start heating the reaction tube to remove the water and acetonitrile in the system. After evaporating to dryness, continue to add 0.5 ml of anhydrous acetonitrile to the reaction flask, and heat and evaporate to dryness again.

[0049] (4) Add BrC dissolved in o-dichlorobenzene 2 h 4 OTf (20 μl BrC 2 h 4 OTf is dissolved in 1.0ml o-dichlorobenzene...

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Abstract

The invention provides a method for synthesizing <18>F ethyl choline and relates to a preparation method of a medical imaging agent. The method comprises the steps of reacting by virtue of 2-bromine ethyl trifluoromethanesulfonate (BrC2H4OTf) and <18>F, so as to generate BrC2H418F, reacting by virtue of BrC2H418F and N,N-dimethylethanolamine, and purifying, so as to obtain the product. The method has the beneficial effects that the reaction process is mild, each reaction step is easily controlled, the requirement on synthetic module equipment is low, the synthetic time is short, and the clinical application of <18>F ethyl choline (<18>F-FECH) is benefited; the reaction yield of a reaction route is high, production equipment and process are simple and are easy in operation, the reaction temperature is low, and the energy consumption is low, so that the production cost is lowered; no exhaust gas is emitted in the preparation process, so that the production is safe; and the whole synthetic process is full-automatically finished by virtue of a synthetic module in a lead-production synthesis hot chamber without human intervention, so that the radiation risk is avoided.

Description

technical field [0001] The invention relates to a method for preparing a medical imaging agent, in particular to a synthetic 18 F Ethylcholine method. Background technique [0002] PET-CT uses radionuclides that emit positrons as emitters, called positron emission computed tomography. PET is the most advanced imaging equipment in the field of nuclear medicine and is regarded as an epoch-making milestone in the history of nuclear medicine. , is a symbol of the highest level of nuclear medicine, and it plays a very important role in tumor diagnosis. 18 F-FDG is currently the most widely used tumor imaging agent. It plays a role in the diagnosis of many tumors, but some tumors use 18 F-FDG can not draw a clear conclusion, and some tumors cannot even be used 18 F-FDG for diagnosis. Therefore, the development of tumor imaging agents with strong specificity and high sensitivity has become a very urgent task. Choline is one of the components of the cell membrane, and the mali...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C213/00C07C215/40
CPCC07C213/00C07B2200/05C07C215/40
Inventor 陈尚东程亮郭振伟
Owner SHENYANG INSTITUTE OF CHEMICAL TECHNOLOGY
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