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Labeling method for hydroxytamine transporter imaging agent [<18>F]-FPBM

A technology of serotonin and labeling method, which is applied in the directions of organic chemical methods, chemical instruments and methods, and preparation of thioether. High efficiency, the effect of improving productivity

Inactive Publication Date: 2012-06-27
BEIJING NORMAL UNIVERSITY
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Problems solved by technology

Since this method involves the reduction of nitro groups, the chemical reagents used are complicated to operate, and it is impossible to realize automatic synthesis conveniently, and the labeling yield is low (~10%)

Method used

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  • Labeling method for hydroxytamine transporter imaging agent [&lt;18&gt;F]-FPBM
  • Labeling method for hydroxytamine transporter imaging agent [&lt;18&gt;F]-FPBM
  • Labeling method for hydroxytamine transporter imaging agent [&lt;18&gt;F]-FPBM

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Embodiment Construction

[0057] this invention[ 18 The preparation method of F]-FPBM comprises the following specific steps:

[0058] first step:[ 18 F] Preparation of KF / K222

[0059] Adsorbed on QMA (4-(4-methylpiperidine) pyridine anion exchange resin) column 18 f - Use 1.1ml eluent [11mg K222 and 2mg K 2 CO 3 acetonitrile / water (0.83mL / 0.17mL)], and the resulting solution was evaporated to dryness in an oil bath at 110°C under nitrogen flow conditions. After evaporation, 1 mL of anhydrous acetonitrile was added, and the solvent was evaporated to dryness under the same conditions. times get dry [ 18 F] KF / K222, slightly cooled for about 1min.

[0060] The second step: [ 18 F] Preparation of labeled intermediate 2

[0061] Dissolve 2mg of 1,3-di-p-toluenesulfonylpropane in 1ml of anhydrous acetonitrile, add the above dry [ 18 F] KF / K222. Shake well and place in an environment of 85-90°C for 5-15 minutes.

[0062] Two key factors in this step:

[0063] 1) Reaction time: the experimental ...

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Abstract

The present invention relates to a labeling method for a hydroxytamine transporter imaging agent [<18>F]-FPBM. According to the method, a <18>F labeling treatment is performed on 1,3-di-p-toluenesulfonyl propane; the resulting labeled intermediate 1-fluoro(<18>F)-3-p-toluenesulfonyl propane reacts with 2-aminobenzene-(2-(N,N-dimethyl)-4-hydroxy)-phenylsulfide to obtain the [<18>F]-FPBM, wherein the reaction process is represented by the following. According to the present invention, the precursor compound 2-aminobenzene-(2-(N,N-dimethyl)-4-hydroxy)-phenylsulfide is firstly used for label of the FPBM, the results show that the compound provides good selectivity for the small molecular chain linking reaction, and the total labeling yield of the labeling method is 13-25%. With the present invention, the optimization of the radioactive synthesis process of the compound is solved, the labeling yield is improved, the automation synthesis is firstly achieved, and the basis is established for the clinical application of the [<18>F]-FPBM in the future.

Description

technical field [0001] The present invention relates to a fluorine-18 labeling method, relates to a new labeling method and a new labeling precursor compound of a class of compounds, and particularly relates to a serotonin transporter imaging agent[ 18 F]-FPBM, that is, fluorine-18 labeled 2-aminobenzene-(2-(N,N-dimethyl)-4-(3-fluoropropyl)-phenyl)sulfide ([ 18 F]-FPBM) labeling method and precursor preparation. Background technique [0002] Serotonin (5-HT) participates in many important regulatory functions of the central nervous system, and affects the body's sleep, appetite, memory, learning ability, body temperature regulation, and mood. It is generally believed that serotonin in the synaptic gap is low Abnormal levels are directly related to psychiatric diseases such as anxiety and schizophrenia, so finding imaging agents that can characterize serotonin levels has important clinical value. This kind of imaging agent can not only help judge the curative effect and est...

Claims

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Application Information

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IPC IPC(8): C07C323/37C07C319/20C07B59/00C07C309/73C07C303/30
Inventor 朱霖李根薰李崧乔晋萍
Owner BEIJING NORMAL UNIVERSITY
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