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Positron emitting tracer, preparation method an applicationthereof

A reaction and compound technology, which is applied in the field of medicine and its preparation, can solve problems such as interference with quantitative analysis of PET images, molecular structure instability, etc.

Active Publication Date: 2017-06-20
广东安迪科正电子技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

therefore,[ 18 F] The instability of the molecular structure of DPA-714 seriously interferes with the quantitative analysis of PET images

Method used

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  • Positron emitting tracer, preparation method an applicationthereof
  • Positron emitting tracer, preparation method an applicationthereof
  • Positron emitting tracer, preparation method an applicationthereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0107] This embodiment provides a kind of compound [ 18 F] FDPA has the following structure:

[0108]

[0109] Chemical name: N, N-diethyl-2-(2-(4-(fluoro18-fluorophenyl))-5,7 dimethylpyrazol[1,5-a]pyrimidine)-3- base) acetamide

[0110] Molecular formula: C 20 h 23 18 FN 4 o

[0111] Molecular weight: 353.43

[0112] This compound can be used as a positron drug targeting the translocation protein TSPO.

Embodiment 2

[0114] This embodiment provides [ 18 F] the preparation method (manual preparation) of FDPA comprises the steps:

[0115] Step 1: Preparation of bare ring prosthetic group SPIAd

[0116] Add 5.0 g of malonic acid (CAS: 141-82-2, product number: A11526-100g) to 4.8 mL of acetic anhydride (Chengdu Huaxia reagent, CAS108-24-7, product number H1133817-500 mL), followed by 24 μL of concentrated sulfuric acid , the temperature of the reaction system was raised to 60° C. for 15 minutes and then cooled to room temperature.

[0117] Slowly add the above reaction system to 48mmol 2-adamantanone (Alfa Aesar, CAS 700-58-3, product number: A14275-100g), and the addition can be completed within about half an hour to one hour, and then evaporated to dryness under pressure Solvent, to obtain the bare ring prosthetic group SPIAd initial product, the bare ring prosthetic group SPIAd initial product was dissolved in 300mL anhydrous ether, backwashed with water three times, each 200mL, the orga...

Embodiment 3

[0157] This example provides [ 18 F] FDPA synthesis system, such as figure 1 shown, including:

[0158] Fluorine-18 negative ion generator;

[0159] Fluorine-18 negative ion eluting device;

[0160] feeding device;

[0161] reaction device;

[0162] HPLC purification device;

[0163] Extraction and collection devices;

[0164] And valve v1, valve v3, valve v5, valve v6, valve v7, valve v8, valve v10, valve v13, valve v18, valve v20, valve v24, and valve v25.

[0165] The fluorine-18 negative ion generating device includes a GE cyclotron and a helium generator, and the GE cyclotron is connected to the QMA solid-phase extraction column of the eluting device through the helium generator through the valve v10,

[0166]The fluorine-18 negative ion eluting device includes an eluent generator and a QMA solid-phase extraction column, the eluent generator is a vial 1, and the vial 1 is connected up and down with the QMA solid-phase extraction column through valves v1 and v10 in ...

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Abstract

The invention provides a novel positron tracer [18F] FDPA of targeting TSPO marked by radioactivefluorine-18, and also provides a marking method and application of a carrier-freeradioactivefluorine-18anion of the [18F]FDPA. The [18F]FDPA provided by the invention has high chemical and radiochemical purity, high specific activity and good repeatability, and meets the quality standard of the positron tracer for injection use; a preparation method of the [18F] FDPA provided by the invention is not only few in steps and high in yield, but also simple and convenient to operate, and easy for automatic production; when the [18F] FDPA is applied in PET imaging evaluation in an inflammation animal model, the [18F] FDPA has good specifity, target-specific action and stability, so that the quality of quantitative analysis of PET images is greatly improved, and a great scientific support is provided for follow-up diagnosis of clinicinflammatory diseases.

Description

technical field [0001] The invention relates to the field of medicine and its preparation method, in particular to a positron radioactive medicine, its preparation method and its application. Background technique [0002] The translocation protein TSPO is a hydrophobic protein encoded by the nucleus and contains 169 amino acids (rich in tryptophan). It is highly expressed in tissues related to body synthesis, such as adrenal gland, gonad, salivary gland, etc. It is also partially expressed in kidney and heart tissue, while the expression level is very low in liver and brain. Studies have shown that TSPO is an important part of steroid hormone synthesis, which can promote the transmembrane transport of cholesterol into phospholipid membranes, increase the formation of pregnenolone and downstream neurosteroid synthesis, repair damaged nerves and promote nerve growth. In addition, TSPO is also involved in many physiological functions, such as cell proliferation, immune respons...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K51/04A61K101/02
CPCA61K51/0459C07B2200/05C07D487/04
Inventor 王璐
Owner 广东安迪科正电子技术有限公司
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