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Receptor molecularly-targeted imaging agent and preparation method and application thereof

A molecular targeting and imaging agent technology, applied in the field of medical imaging, can solve the problems of reducing the fat solubility of F-FES, increasing the fat solubility, and limiting the development of probes, and achieves good chemical stability and biodistribution properties, specific activity. The effect of high degree and simple and easy preparation method

Active Publication Date: 2017-05-10
XIAMEN UNIV
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Problems solved by technology

right 18 There are many examples of F-FES configuration modifications, but none of these modifications have really reduced 18 The fat solubility of F-FES, and some even increase its fat solubility, these properties limit the development of this type of probe

Method used

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  • Receptor molecularly-targeted imaging agent and preparation method and application thereof
  • Receptor molecularly-targeted imaging agent and preparation method and application thereof
  • Receptor molecularly-targeted imaging agent and preparation method and application thereof

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Embodiment Construction

[0033] The following is a further illustration and description of the technical solution of the present invention through the specific implementation of compound 5 in conjunction with the accompanying drawings.

[0034] 1. Preparation of compound 5

[0035] 1) Synthesis of compound 2:

[0036] At 0°C, 1.5g of compound 1 and 1.7mL of triethylamine were dissolved in 10mL of dichloromethane, 4.77g of p-toluenesulfonyl chloride was added, and reacted at room temperature for 5 hours. After the reaction, the reaction solution was extracted three times with dichloromethane, the organic phase was collected and the solvent was removed by rotary evaporation. The product was passed 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.

[0037] 2) Synthesis of Compound 3:

[0038]Completely dissolve 0.65g of sodium azide in 10mL of N,N-dimethylformamide, add 4.59g of compound 2, and stir at roo...

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Abstract

The invention discloses a receptor molecularly-targeted imaging agent and a preparation method and application thereof. The receptor molecularly-targeted imaging agent comprises a polyethylene glycol short chain which is linked with 17alpha-ethinyloestradiol of a target estrogen receptor through 'click' reaction. The receptor molecularly-targeted imaging agent is shown as a concrete general molecular formula in the description, wherein the 17alpha-ethinyloestradiol serves as a targeting group, polyethylene glycol serves as a hydrophilic group, and <18>F serves as a radioactive group. The receptor molecularly-targeted imaging agent has excellent biological properties and high specificity, is high in uptake when used in positive breast cancer tumors of the estrogen receptor and capable of distinguishing between estrogen positive receptors and estrogen negative receptors, and meets the conditions as a breast cancer receptor imaging agent.

Description

technical field [0001] The invention belongs to the technical field of medical imaging, and in particular relates to a receptor targeting imaging agent and a preparation method thereof. Background technique [0002] Breast cancer is a serious threat to women's health and life. According to cancer statistics in 2015, the incidence of breast cancer ranks first among female malignant tumors. Early diagnosis is the key to treating breast cancer. In 1978, Lippman et al. concluded through experiments that about 70%-80% of breast cancer patients overexpress estrogen receptors. Today, the distribution and level of estrogen receptors is one of the key prognostic factors for breast cancer. Clinically, the dosage of anti-estrogen drugs for patients is determined according to the status of estrogen receptors. [0003] At present, pathological methods are mainly used clinically to detect and quantify breast cancer receptor types. This method of pathological slicing requires invasive o...

Claims

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Application Information

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IPC IPC(8): C07J43/00C07B59/00A61K51/06A61K101/02
CPCA61K51/06C07B59/007C07B2200/05C07J43/003
Inventor 张现忠许多庄荣强尤林怡郭志德张德良张蒲
Owner XIAMEN UNIV
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