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A sort of 18 Automatic preparation method and device for f-(2S,4R)-4-fluoro-L-glutamine

A technology of glutamine and fluorination reaction, which is applied in the field of automatic preparation and device of 18F-(2S,4R)-4-fluoro-L-glutamine, which can solve the problems of difficult contact, poor material corrosion resistance, corrosion And other issues

Active Publication Date: 2017-04-19
BEIJING INST FOR BRAIN DISORDERS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But if used for 18 The preparation of F-(2S,4R)-4-FGln still has the following problems: First, it has not yet developed a 18 F-(2S,4R)-4-FGln prepared special-purpose disposable tubing and ferrule; second, the materials used in disposable tubing have poor corrosion resistance and are not easy to contact organic acids such as trifluoroacetic acid; 3. There is no waste gas treatment device for volatile organic acids, and the use of organic acids such as trifluoroacetic acid will cause the device to be corroded
The advantage of this device is that it adopts a pinch-type solenoid valve, so that the preparation reagents flow in the pipeline, avoiding the residue in the valve body and the corrosion of the valve body; the disadvantage is that there is no tail gas treatment system, and the use of volatile organic acids will cause cause corrosion of the device, so the BNU F-A2 type cannot be applied to 18 Preparation of F-(2S,4R)-4-FGln

Method used

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  • A sort of <sup>18</sup> Automatic preparation method and device for f-(2S,4R)-4-fluoro-L-glutamine
  • A sort of <sup>18</sup> Automatic preparation method and device for f-(2S,4R)-4-fluoro-L-glutamine
  • A sort of <sup>18</sup> Automatic preparation method and device for f-(2S,4R)-4-fluoro-L-glutamine

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0112] Embodiment 1 (carried out intermediate purification by reverse-phase purification cartridge):

[0113] 18 Preparation of F-(2S,4R)-4-fluoro-L-glutamine.

[0114] Items and materials:

[0115] Contains H 18 The aqueous solution of F was prepared by the Cyclone-10 medical cyclotron accelerator of IBA Company, with a radioactivity of 29.6 GBq; 18-crown-6, KHCO 3 , acetonitrile, ethanol, trifluoroacetic acid, anisole (which is used to prepare the trifluoroacetic acid solution containing 0.5% anisole), copper sulfate pentahydrate and other chemical reagents were purchased from Sigma-Aldrich Company and Beijing Chemical Plant, purity All are of reagent grade and used directly without instructions; anion exchange Spe Pak QMA column, solid phase extraction Spe Pak C-18 column, Oasis HLB column, ion adsorption alumina column were purchased from Waters; SAX strong anion exchange column was purchased from Alltech Company; sterile filter membrane purchased from Merck Millipore ...

Embodiment 2

[0146] Example 2 ( 18 F-(2S,4R)-4-fluoro-L-glutamine automatic preparation process optimization)

[0147] use 18 Optimization of automatic preparation device for F-(2S,4R)-4-fluoro-L-glutamine 18 Preparation process of F-(2S,4R)-4-fluoro-L-glutamine.

[0148] improved 18 Phase transfer catalyst 18-crown-6 / KHCO in the preparation process of F-(2S,4R)-4-fluoro-L-glutamine 3 Solution drying process, precursor compound dosage and final product purification method optimization.

[0149] Phase transfer catalyst 18-crown-6 / KHCO 3 The drying of the solution is carried out by the azeotropic evaporation of acetonitrile and water. The number of repeated additions of acetonitrile and evaporation affects the drying effect, and the drying process takes a long time, which has a great impact on the production yield.

[0150] The optimization method is:

[0151] 1) Evaporate and dry once: use 18-crown-6 / KHCO in device vial 1 3 (also amino polyether K 222 / K 2 CO 3 solution or TBAHCO...

Embodiment 3

[0161] preparation 18 The purification of intermediates in the F-(2S,4R)-4-fluoro-L-glutamine process can be implemented by high performance liquid chromatography, and the semi-preparative high-pressure liquid chromatography system (HPLC) used is the Belgian IBA company's Synthera HPLC system. The Synthera HPLC system can be loaded with two mobile phases and contains an on-line UV detector and an on-line radioactivity detector. The connection method is as follows: connect the outlet end of the electromagnetic valve 39 of the synthesis device with the sample loop of the HPLC system, and connect the outlet of the mobile phase collected by the HPLC to the vial 8 .

[0162] preparation 18 The preparation work of F-(2S,4R)-4-fluoro-L-glutamine is as follows: connect the normally open end liquid inlet of solenoid valve 37 with that of Cyclone-10 type medical cyclotron 18 f - The solution is exported to the pipeline connection; the common gas inlet of the device electromagnetic v...

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Abstract

The invention relates to an automatic preparation method and device for <18>F-(2S,4R)-4-fluoro-L-glutamine. The method comprises the following steps: (1) capturing fluorinating reagent <18>F<->; (2 ) preparing <18>F<-> with nucleophilic reactivity; (3) carrying out a fluorination reaction; (4) purifying an intermediate; (5) carrying out an intermediate deprotection reaction; (6) carrying out purification and preparation of a product, wherein allowing a crude product solution obtained in the step (5) to pass a purification and preparation unit to prepare a <18>F-(2S,4R)-4-fluoro-L-glutamine product solution. Through the adoption of the automatic preparation method and device for <18>F-(2S,4R)-4-fluoro-L-glutamine, automatic preparation of <18>F-(2S,4R)-4-fluoro-L-glutamine is realized, the preparation efficiency and the stability are improved, meanwhile, an operator is protected from radiation damage, and the foundation is laid for clinical application of <18>F-(2S,4R)-4-fluoro-L-glutamine as a new metabolic imaging agent.

Description

technical field [0001] The invention relates to a method and device for automatic labeling preparation and purification of positron emission tomography (PET) drugs, in particular to a 18 An automatic preparation method and device for F-(2S,4R)-4-fluoro-L-glutamine [(2S,4R)-2,5-diamino-4-fluoro-5-oxopentanoic acid]. Background technique [0002] Positron emission tomography (PET) is an imaging method that has been widely used clinically. Its principle is to reflect the physiological and pathological changes of specific targets by detecting the distribution of positron drugs in the human body. For disease diagnosis and research. Positron drugs are the key to the function of PET. These drugs are labeled with medical positron nuclides and can participate in specific physiological processes or bind to specific targets after entering the human body. [0003] The most widely used radiopharmaceutical is 2- 18 F-2-deoxy-D-glucose ([ 18 F]FDG), mainly used for tumor diagnosis, cla...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C237/06C07C231/12C07B59/00
Inventor 朱霖孔繁渊张岩乔洪文查智豪吴泽辉
Owner BEIJING INST FOR BRAIN DISORDERS
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