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EGFR positron tracer, preparation method and application thereof

A technology of positron tracer and PET imaging agent, which can be used in pharmaceutical formulations, in vivo radioactive preparations, preparations for in vivo experiments, etc., can solve the problems of short C half-life, difficult to study large specimens, and limited number of patients, etc. To achieve the effect of convenient preparation method, meeting the needs of scientific research and clinical trials, and good tracer effect

Inactive Publication Date: 2015-08-05
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV +1
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Problems solved by technology

[0006] Although in recent years scholars have used 11 C-Erlotinib has achieved many achievements in basic research and clinical research, but there are also some shortcomings that limit its further application: (1) 11 C has a short half-life, making it difficult to conduct large-scale research
(2) 11 C-Erlotinib can only be used in PET / CT centers with accelerators, and the number of patients that can be satisfied by a single production is limited (the dose of each production can only satisfy a maximum of 3 patients)
Although there is currently no information on the 18 F-erlotinib related research reports, but based on the above reasons, 18 F-Erlotinib is the most promising to be widely used as a supplement in the future clinical 18 F-FDG tumor imaging is used for tumor diagnosis, and at the same time guides clinical personalized treatment of positron imaging agents, and is expected to make certain contributions in the biomedical industry

Method used

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  • EGFR positron tracer, preparation method and application thereof
  • EGFR positron tracer, preparation method and application thereof
  • EGFR positron tracer, preparation method and application thereof

Examples

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preparation example Construction

[0028] The preparation method of EGFR positron tracer comprises the steps:

[0029] 1) Dissolving 2-azidoethyl p-toluenesulfonate in an organic solvent to obtain a 2-azidoethyl p-toluenesulfonate solution for subsequent use;

[0030] 2) Erlotinib is dissolved in a solvent to obtain an Erlotinib solution, which is set aside;

[0031] 3) application 18 O water production gets 18 F and conducted in the anion exchange column, the 18 F is rinsed into the reaction bottle;

[0032] 4) Remove the water in the reaction flask and dry 18 F / 19 F, adding 2-azidoethyl p-toluenesulfonate solution to react, distilling out the reaction product after the reaction to obtain a light yellow liquid;

[0033] 5) Add the Erlotinib solution and an appropriate amount of catalyst into the light yellow liquid, and the reaction is complete;

[0034] 6) Add water to dilute the reaction product, pass through the Sep-Par C-18 column, then rinse the C-18 column with water, dry it and rinse the C-18 co...

Embodiment 1

[0047] 1) Application of medical cyclotron bombardment 18 O water, through 18 O(p n) 18 F nuclear reaction produces 500mCi 18 F, and conduct in anion exchange column, measure activity and use 1mL mixed solution (12.0mg 4,7,13,16,21,24-hexaoxo-1,10-diazabicyclo[8.8.8]26 Alkane (K 2.2.2. ) plus 3.0mgK 2 CO 3 dissolved in 0.1mL water and 0.9mL acetonitrile) will 18 F is rinsed into the reaction bottle;

[0048] 2) Continuously blow high-purity helium into the reaction bottle, azeotropically remove water at 110°C, and blow dry; dissolve 5 mg of precursor 1 (2-azidoethyl p-toluenesulfonate) in 0.5 mL Add acetonitrile into the reaction bottle, react at 80°C for 10 minutes, and distill a light yellow liquid under reduced pressure after the reaction is completed;

[0049] 3) Dissolve 5 mg of precursor 2 (Erlotinib) in 1 mL of solvent (tert-butanol: water = 1:1) and add an appropriate amount of catalyst (0.05 eq CuSO 4 ·5H 2 O, 0.1eq sodium ascorbate dissolved in 0.5mL water...

Embodiment 2

[0053] 1) Application of medical cyclotron bombardment 18 O water, through 18 O(p n) 18 F nuclear reaction produces 500mCi 18 F, and conduct in anion exchange column, measure activity and use 1mL mixed solution (12.0mg 4,7,13,16,21,24-hexaoxo-1,10-diazabicyclo[8.8.8]26 Alkane (K 2.2.2. ) plus 4.3mg KHCO 3 dissolved in 0.1mL water and 0.9mL acetonitrile) will 18 F is rinsed into the reaction bottle;

[0054] 2) Continuously blow high-purity helium into the reaction bottle, azeotropically remove water at 110°C, and blow dry; dissolve 5 mg of precursor 1 (2-azidoethyl p-toluenesulfonate) in 0.5 mL Add acetonitrile into the reaction bottle, react at 80°C for 10 minutes, and distill a light yellow liquid under reduced pressure after the reaction is completed;

[0055] 3) Dissolve 5 mg of precursor 2 (Erlotinib) in 1 mL of solvent (tert-butanol: water = 1:1) and add an appropriate amount of catalyst (0.05 eq tris(triphenylphosphine) copper bromide (BrCuP(PPh 3 ) 3 )) into ...

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Abstract

The invention discloses an EGFR positron tracer, a preparation method and application thereof. The structural formula of the EGFR positron tracer is shown as the specification. The EGFR positron tracer has good tracing effect, and compared with 18F-FDG that is the most common in clinical practice at current, the tracer has very good specificity, can achieve positive identification of epidermal growth factor receptor (EGFR) high expression tumors. The preparation method is convenient, simple and fast, can realize fully automatic production, and can meet scientific research and clinical demands. In the aspect of application, the PET imaging of 18F-Erlotinib not only can be used for screening of clinical anticancer drug Erlotinib sensitive individuals, and also has very good application prospects in detection of EGFR expression level and screening of small molecule EGFR inhibitors in the pharmaceutical industry.

Description

technical field [0001] The invention relates to an epidermal growth factor receptor (EGFR) positron tracer and its preparation method and application. Background technique [0002] Positron Emission Tomograghy ​​(PET) is currently the best imaging device for monitoring the occurrence and development of tumors in vivo. Non-invasive, three-dimensional, and dynamic research on physiological and biochemical processes. PET can be applied to tumor diagnosis, differentiation of benign and malignant tumors, malignant tumor staging, typing, early diagnosis and identification of tumor recurrence and metastasis, selection of treatment options and the effects of chemotherapy and radiotherapy The detection of the tumor and the observation of the process of tumor changes and the monitoring of the prognosis. PET examination relies on the specific metabolism, absorption, and binding of broad-spectrum or specific targeted positron imaging agents in target organs. 18 F-FDG is currently the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/10A61K51/04A61K101/02
CPCA61K51/0459C07D403/10
Inventor 黄顺王全师郑希张焜杜志云韩彦江吴湖炳王猛孙朋辉
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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