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Estrogen receptor targeting radioactive tracer, and preparation method and application thereof

A radiotracer and estrogen receptor technology, which is applied in the field of medical imaging and achieves the effects of low non-specific background, excellent in vivo biological properties, and a simple and easy preparation method

Active Publication Date: 2020-07-14
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Compared with other multi-step radiolabeling methods, the single-step iodine labeling method is easier to apply and promote, and there is no research using this method for ER imaging agent labeling

Method used

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  • Estrogen receptor targeting radioactive tracer, and preparation method and application thereof
  • Estrogen receptor targeting radioactive tracer, and preparation method and application thereof
  • Estrogen receptor targeting radioactive tracer, and preparation method and application thereof

Examples

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Embodiment 1

[0042] A preparation method of an estrogen receptor targeting radiotracer (compound 6) of the present embodiment, comprising the following steps:

[0043] 1) Synthesis of compound 2:

[0044] First place the reaction device in an ice-water bath, then dissolve 1.5g of compound 1 and 1.7mL of triethylamine in 10mL of dichloromethane, and finally add 2.29g of p-toluenesulfonyl chloride dissolved in 20mL of dichloromethane, first 0 °C for 1 hour, and then at room temperature for 5 hours. After the reaction, the product was washed with water and the reaction solution was extracted three times with dichloromethane, the organic phase was collected and the solvent was removed by rotary evaporation. The crude product was purified through a silica gel column, and the mobile phase ratio was petroleum ether: ethyl acetate = 2:1. Compound 2 was obtained as pure white crystals.

[0045] 2) Synthesis of compound 3:

[0046] At room temperature, add 0.65g of sodium azide into 10mL of N,N-...

Embodiment 2

[0076] A preparation method of an estrogen receptor targeting radiotracer (compound 8) of the present embodiment, comprising the following steps:

[0077] Add 1mg of compound 7 into a 5mL microwave reaction tube, then add 0.1mL of acetonitrile as a solvent, and finally add 0.1mL of fluorine-18 aqueous solution, and react with microwave at 180°C for 10 minutes. After the reaction was completed, HPLC purification was performed. HPLC conditions are: mobile phase A is water, phase B is acetonitrile: 0 to 10 minutes: 35% B, 10 to 20 minutes: 60% B, 20 to 30 minutes: 35% B; the flow rate is 1 mL / min. The HPLC analysis chart of purified compound 8 and its non-radioactive standard reference compound is as follows: figure 2 As shown, the peak times of the two are similar, which proves the correctness of compound 8 labeling.

[0078] Compound 8 in this example is labeled with the standard reference compound of Compound 6 as a precursor, and the labeling method is simple and easy. Fr...

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Abstract

The invention discloses an estrogen receptor targeting radioactive tracer, and a preparation method and application thereof. The tracer is of an ethinylestradiol dimer structure, molecules of the tracer comprise two same 17 alpha-ethinylestradiol groups, and the tracer is prepared by marking radioactive signal groups in one step through a polyethylene glycol short chain by applying a click chemical reaction. The tracer has high uptake in uterus, ovary, breast cancer cells and tumors with positive estrogen receptors, can distinguish estrogen positive receptors from estrogen negative receptors in vitro and vivo, has strong specificity, and meets the condition of being used as a breast cancer estrogen receptor imaging agent. The structural formula of the tracer is shown as follows.

Description

technical field [0001] The invention belongs to the technical field of medical imaging, and in particular relates to an estrogen receptor targeting radiotracer, a preparation method and an application. Background technique [0002] Although the mortality rate of breast cancer has decreased with the continuous development of medical level in recent years, breast cancer is still the main cause of death of women worldwide. Statistics show that about 70-80% of breast cancers are estrogen receptor (ER) positive, and ER-positive breast cancers grow slower, better differentiated, and have a slightly better overall prognosis than breast cancers with other receptor types . Therefore, whether ER expression has become one of the few prognostic factors, together with axillary lymph node status, tumor size and histological grade, guide clinical treatment of breast cancer. Especially for guiding endocrine therapy, breast tumors with low levels of ER tend to respond poorly to endocrine t...

Claims

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Application Information

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IPC IPC(8): A61K51/04C07J43/00A61K101/02
CPCA61K51/0412C07J43/003
Inventor 张现忠许多彭晨钰高菲郭志德庄荣强
Owner XIAMEN UNIV
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