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Preparation process of positron imaging agent 18F-5-floro-N-(2-(diethylamino) ethyl) pyridinecarboxamide

A technology of 18F-5- and positron imaging agents, applied in the direction of radioactive carriers, etc., can solve the problems of difficulty in obtaining stable output, long process time, and large radiation dose, and achieve easy automatic operation and simple preparation process , the effect of high sensitivity

Inactive Publication Date: 2015-05-27
XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV
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Problems solved by technology

Currently 18 F-5-fluoro-N-(2-(diethylamino) ethyl) pyridinecarboxamide is limited to laboratory traditional chemical method synthesis and purification, the whole operation is carried out manually, the process is complicated and takes a long time (2~3 hours), causing a large radiation dose to the operator
For the sake of radiation safety, the reaction in the laboratory synthesis process 18 f - The radioactivity of the ion should not be too high, the process takes too long and the radioactivity decays more, and the radioactivity of the obtained product is low (1-2mCi), which can only meet the dose required for small animal experiments, and it is difficult to guarantee the success of each experiment get a steady output
Based on the above, the laboratory synthesis process cannot meet the clinical requirements, which hinders the 18 Clinical application of F-5-fluoro-N-(2-(diethylamino)ethyl)pyridinecarboxamide

Method used

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  • Preparation process of positron imaging agent 18F-5-floro-N-(2-(diethylamino) ethyl) pyridinecarboxamide
  • Preparation process of positron imaging agent 18F-5-floro-N-(2-(diethylamino) ethyl) pyridinecarboxamide
  • Preparation process of positron imaging agent 18F-5-floro-N-(2-(diethylamino) ethyl) pyridinecarboxamide

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Embodiment 1

[0032] provided by the invention 18 The synthetic route of F-5-fluoro-N-(2-(diethylamino) ethyl) pyridinecarboxamide is as follows figure 1 Shown, the precursor is 5-bromo-N-(2-(diethylamino) ethyl) pyridine carboxamide, can refer to literature (Liu, H.et al., Development of[ 18 F]-labeled picolinamide probes for PET imaging of malignant melanoma. J Med Chem, 2013, 56, 895-901) synthesis.

[0033] provided by the invention 18 The pipeline diagram of the preparation process of F-5-fluoro-N-(2-(diethylamino)ethyl)pyridinecarboxamide is attached figure 2 As shown, the specific process is as follows:

[0034] 1. Preparation before automatic synthesis:

[0035] 1. Short-circuit the valve V17 and valve V15 in the pipeline.

[0036] 2. Add 0.6ml of eluent to the container bottle controlled by valve V1, the eluent uses 2.8mgK 2 CO 3 , 12mg phase transfer catalyst kryptofix.k222, 300μl sterile water and 1ml acetonitrile configuration;

[0037] Add 5 mg of the precursor 5-bromo...

Embodiment 2

[0048] The present invention has investigated the preparation of the embodiment of the present invention 1 18 The cell uptake of F-5-fluoro-N-(2-(diethylamino)ethyl)pyridinecarboxamide, the specific steps are as follows: Take B16F10 and A375m cells in logarithmic growth phase and plate them, 1×10 per well 5 cells. Added to each well 18 F-5-fluoro-N-(2-(diethylamino)ethyl)pyridinecarboxamide (2μCi / well) set 3 duplicate wells in each group, incubate at 37°C for 30min, 60min and 120min respectively, absorb the radioactive medium , washed twice with PBS and collected in the same test tube. Cells were lysed with 1N NaOH and then washed twice with PBS and collected in the same test tube. Finally, the radioactive counts of the supernatant and cell lysate were measured with an automatic gamma counter. Results are expressed as cellular uptake rates:

[0049] Cell uptake rate (%)=Counts cell lysate / (Counts cell lysate+Counts supernatant)×100%.

[0050] for cell blocking studiesfor ...

Embodiment 3

[0056] The present invention utilizes the tumor-bearing mouse model to investigate the preparation of the embodiment of the present invention 1 18 PET imaging and blocking imaging of F-5-fluoro-N-(2-(diethylamino)ethyl)pyridinecarboxamide, the specific steps are as follows:

[0057] Animal tumor model construction: C57BL / 6 mice (female, 5-6 weeks old) and BALB / C nude mice (female, 3-4 weeks old) were provided by Beijing Huafukang Biotechnology Co., Ltd. There is no special pathogen barrier system in the experimental center. All animals used in the experiment were approved by the Experimental Animal Use and Management Committee of Tongji Medical College, Huazhong University of Science and Technology. B16F10 cells 2×10 5 Suspended in 150 μl PBS, planted subcutaneously in the axilla of the right upper limb of C57BL / 6 mice, A375m cells in 2×10 6 One was suspended in 150 μl of PBS, subcutaneously planted in the armpit of the right upper limb of nude mice, and can be used for ani...

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Abstract

The invention provides a preparation process of 18F-5-floro-N-(2-(diethylamino) ethyl) pyridinecarboxamide. The preparation process comprises the following steps: S1, capturing 18F-F<->; S2, dehydrating; S3, marking; and S4, purifying. The preparation process is simple, rapid and easy to automatically operate, and a target compound can be stably prepared. The 18F-5-floro-N-(2-(diethylamino) ethyl) pyridinecarboxamide provided by the invention is a positron imaging agent for diagnosing and periodizing malignant melanoma and is high in targeting, specificity and binding force with melanin; the imaging agent is quickly excreted through the kidney, rapid to shoot the tumor part, high in tumor / normal tissue ratio and good in imaging quality; and the imaging agent is high in sensitivity and can be used for detecting micro metastatic lesions. The preparation process of 18F-5-floro-N-(2-(diethylamino) ethyl) pyridinecarboxamide provided by the invention provides a basis for clinically diagnosing and periodizing malignant melanoma.

Description

technical field [0001] The present invention relates to the application field of PET (Positron Emission Tomography, positron emission tomography imaging), in particular to a novel positron imaging agent targeting malignant melanoma 18 F-5-fluoro-N-(2-(diethylamino) ethyl) pyridinecarboxamide ( 18 F-5-FPN) preparation technology and application. Background technique [0002] Malignant melanoma (Maligna melanoma, MM) is a malignant tumor originating from melanocytes. It has a high degree of malignancy, is prone to metastasis, and has a high recurrence rate. The incidence rate has gradually increased in recent years. Although the incidence of malignant melanoma only accounts for 3% of all malignant skin tumors, its mortality rate is more than 75%, and its prognosis and survival rate are closely related to clinical stages (Siegel, R. et al., Cancer treatment and survival statistics, 2012. CA Cancer J Clin, 2012, 62, 220-41; Jemal, A. et al., Cancer statistics, 2009. CA Cancer ...

Claims

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Application Information

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IPC IPC(8): A61K51/04A61K101/02
Inventor 兰晓莉冯洪燕柳轻瑶覃春霞夏晓天李崇佼张永学
Owner XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV
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