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11C-labelled EGFR positron tracer and preparation method and application thereof

A positron tracer, 11C-CH3I technology, applied in organic chemistry, radioactive carriers, etc., can solve the problems of expensive targeted drugs, drug resistance, and heavy burden on patients, and achieve good production efficiency and practical application. The effect of high stability, good radiation protection, and short preparation time

Inactive Publication Date: 2019-06-28
THE FIRST AFFILIATED HOSPITAL OF GUANGZHOU MEDICAL UNIV (GUANGZHOU RESPIRATORY CENT)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, although the response rate of patients with EGFR activating mutations to EGFR-TKIs targeting drugs can reach 70%, the treatment effect on target-negative tumors is often poor, even worse than that of cytotoxic chemotherapy drugs
Targeted drugs are expensive and require multiple courses of treatment, which poses a greater burden on patients
Moreover, after patients have used EGFR-TKIs for a period of time, drug resistance often occurs, and other targeted drugs need to be replaced for treatment

Method used

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  • 11C-labelled EGFR positron tracer and preparation method and application thereof
  • 11C-labelled EGFR positron tracer and preparation method and application thereof
  • 11C-labelled EGFR positron tracer and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] A sort of 11 C-labeled EGFR positron tracer ( 11 C-AZD9291), prepared by the following method:

[0048] S1: 1% O by volume percentage 2 and 99%N 2 The mixed gas is the target gas, after nuclear reaction 14 N(p,α) 11 C is produced with a cyclotron to obtain 200mCi 11 C-CO 2 , adding the above 11 C-CO 2 adsorbed on In molecular sieves, high-purity N 2 Purge to remove other impurity gases.

[0049] By heating molecular sieves, using high-purity N 2 Will 11 C-CO 2 Carried into the synthesizer (GM's TracerLab FX-FC module).

[0050] S2: In the synthesizer, 11 C-CO 2 Under the catalysis of metal Ni, at 400 °C with H 2 react, produce 11 C-CH 4 . 11 C-CH 4 at 720°C with I 2 react, produce 11 C-CH 3 I, 11 C-CH 3 I reacts with AgOTf at 200°C to generate 11 C-Methyltriflate.

[0051] S3: The precursor AZD7550 (N-(4-methoxy-2-(methyl(2-(methylamino)ethyl)amino)-5-((4--(1-methyl-1H-indol-3-yl)pyrimidin -2-yl)amino)phenyl)acrylamide) was dissolved in 1mL...

Embodiment 2

[0055] Prepared by Example 1 11 The structure of C-AZD9291 was confirmed.

[0056] Identification was performed using analytical high performance liquid chromatography.

[0057] 1. Detection conditions

[0058] Stationary phase: Thermo Synoronis C18 column

[0059] Mobile phase: 0.2% ammonia methanol: water = 90:10 (v:v);

[0060] Flow rate: 1mL / min;

[0061] UV detector detection wavelength: 254nm;

[0062] Gamma radioactivity detector: Bioscan FC-3600.

[0063] 2. Results

[0064] figure 1 for 11 C-AZD9291 and standard AZD9291 high performance liquid chromatography, where: A: 11 C-AZD9291 radioactive chromatogram; B: 11 C-AZD9291 UV chromatogram; C: Standard 12 C-AZD9291 UV chromatogram.

[0065] The results show: 11 The retention time of C-AZD9291 was 8.9min, which was the same as that of the standard 12 The retention time of C-AZD9291 was consistent.

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Abstract

The invention relates to an 11C-labelled EGFR positron tracer and a preparation method and application thereof, and belongs to the technical field of medicinal chemistry. The 11C-labelled EGFR positron tracer is shown in the formula I. The tracer can completely reflect physiological and biochemical processes of clinical medication AZD9291 in cell tissue, by using the tracing effect of positron radionuclide, the pharmaceutical metabolism process in tumor cells and tissue is reflected, and the tracer has an important significance in research on tumor mechanisms, evaluation of medicinal cure effects and treatment monitoring. Especially for positron emission tomography (PET / CT), 11C-labelled AZD9291 is a developer high in practical value.

Description

technical field [0001] The present invention relates to medicinal chemistry and nuclear pharmacy, in particular to a 11 C-labeled EGFR positron tracer and its preparation method and application. Background technique [0002] Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (tyrosine kinase inhibitor, TKI) is a research hotspot in cancer targeted therapy drugs in recent years. The mechanism of EGFR-TKIs targeted therapy is that these molecules can selectively act on tumor cells, bind to the intracellular EGFR tyrosine kinase region, prevent or reduce the phosphorylation of tyrosine kinase, and finally achieve the effect of inhibiting tumor proliferation . [0003] Although EGFR-TKIs targeted therapy has a good therapeutic effect, not all patients are suitable for this strategy. For example, although the response rate of patients with EGFR activating mutations to EGFR-TKIs targeting drugs can reach 70%, the treatment effect on target-negative tumors is ofte...

Claims

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Application Information

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IPC IPC(8): C07D403/04A61K51/04A61K101/00
Inventor 劳业兴甘满权王欣璐
Owner THE FIRST AFFILIATED HOSPITAL OF GUANGZHOU MEDICAL UNIV (GUANGZHOU RESPIRATORY CENT)
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