Automatic preparation method and device for <18>F-(2S,4R)-4-fluoro-L-glutamine

A technology for glutamine and fluorination reaction, which is applied in the field of automatic preparation of 18F-(2S,4R)-4-fluoro-L-glutamine and its device, and can solve the problems of inapplicability, difficult contact, and corrosion resistance of materials. Sexual issues, etc.

Active Publication Date: 2015-12-16
BEIJING INST FOR BRAIN DISORDERS
View PDF8 Cites 5 Cited by
  • 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 trifluoro...

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Automatic preparation method and device for &lt;18&gt;F-(2S,4R)-4-fluoro-L-glutamine
  • Automatic preparation method and device for &lt;18&gt;F-(2S,4R)-4-fluoro-L-glutamine
  • Automatic preparation method and device for &lt;18&gt;F-(2S,4R)-4-fluoro-L-glutamine

Examples

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 29.6GBq; 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 reagent grade, and used directly without instructions; anion exchange SpePakQMA column, solid phase extraction SpePakC-18 column, OasisHLB column, ion adsorption alumina column were purchased from Waters; SAX strong anion exchange column was purchased from Alltech; sterile Filter membranes were purchased from Merck Millipore.

[0116]...

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 (It can also be amino polyether K 222 / K 2 CO 3 solution...

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 SyntheraHPLC system can be loaded with two mobile phases and contains an online UV detector and an online 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 gas inlet shared by the device electromagnetic valv...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

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 in clinical practice. 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, classification and curative effect evaluation. In clinical application, it was found that some tumors [ 18 F] FDG-PET imaging was negative, suggesting th...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap