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<99m>Tc-labeled complex and application thereof in diagnosis of non-small cell lung cancer

A complex and labeling technology, which is applied to compounds of group 7/17 elements of the periodic table, organic compounds of group 7/17 without C-metal bonds, pharmaceutical formulations, etc., to achieve good retention, simple preparation, and high intake Effect

Inactive Publication Date: 2019-08-30
MUDANJIANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the core problem of this technology is how to find an imaging agent that can bind to a certain molecule expressed by tumor cells, select a ligand with high affinity and high specificity, and label it with an appropriate isotope to measure the number and concentration of receptors Changes, to judge the relationship between this change and the disease, to achieve the purpose of diagnosis

Method used

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  • &lt;99m&gt;Tc-labeled complex and application thereof in diagnosis of non-small cell lung cancer
  • &lt;99m&gt;Tc-labeled complex and application thereof in diagnosis of non-small cell lung cancer
  • &lt;99m&gt;Tc-labeled complex and application thereof in diagnosis of non-small cell lung cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1: the preparation of formula (II) compound

[0020]

[0021] In a 500 mL round bottom flask, dissolve 50 g of osimertinib in 250 mL of acetonitrile, add 27 g of anhydrous K 2 CO 3 Stir for 0.5 hours, then add 15.2g of 1-bromopropanol and heat to reflux for 12 hours. After the reaction is completed, add deionized water to quench, extract with dichloromethane, and purify by column chromatography to obtain 44.1g of the compound of formula (II), with a yield of 78.9% , ESI / MS: 558.31[M+H + ].

[0022] Step (2): preparation of formula (III) compound

[0023]

[0024] In a 500mL round-bottomed flask, dissolve 55.7g of the compound of formula (II) in 200mL of DMSO (dimethyl sulfoxide), add 25g of KOH, heat to 100°C for 1 hour, and then dropwise add 10mL of carbon disulfide (CS 2 ), after the TLC detection reaction was completed, the solvent was removed, and ethanol / ether recrystallized to obtain 37.8g of compound of formula (III), yield 56.3%, ESI / MS: 672...

Embodiment 2

[0028] Embodiment 2: adopt HPLC method to identify formula (I) complex

[0029] Kromasil C18 analytical column (4.6×250mm), the mobile phase is water containing 0.1% TFA (trifluoroacetic acid) (phase A) and methanol containing 0.1% TFA (phase B), the flow rate is 1mL / min; t=0, A / B =5 / 5; t=15min, A / B=1 / 9; t=20min, A / B=1 / 9; t=25min, A / B=5 / 5. The retention time (Rt) of the complex of formula (I) is 11.5 min.

[0030] The results of HPLC analysis show that the radiochemical purity of the compound of formula (I) prepared by the above method is greater than 90%.

Embodiment 3

[0031] Embodiment 3: formula (I) complex stability analysis

[0032] The radiochemical purity of the labeled complex of formula (I) was measured after placing it in mouse serum at room temperature and at 37°C for different times (1, 2, 3, 4, 5, 6, 8, 10 hours), Experimental results show that the radiochemical purity of the complex is greater than 90% at room temperature and in mouse serum at 37°C for 10 hours, indicating that it has good stability in vitro.

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Abstract

The invention discloses a <99m>Tc-labeled complex and an application thereof in the diagnosis of non-small cell lung cancer. Specifically, a ligand is formed between osimertinib and CS2, and then theligand and <99m>Tc are subjected to coordination to form a complex of a formula (I). The complex is a hydrophilic complex, the stability is good, the preparation is simple, and the complex has relatively high intake and good retention in lungs, has strong signal intensity, and can be applied in the diagnosis of lung cancer diseases, especially non-small cell lung cancer.

Description

technical field [0001] The invention relates to a 99m technetium-labeled complex and its application in the diagnosis of non-small cell lung cancer, in particular to the complex formed by osimertinib and 99m technetium. Background technique [0002] Lung cancer is the most lethal tumor among malignant tumors, and about 1.5 million people die of lung cancer worldwide every year. The proportion of non-small cell lung cancer (NSCLC) among newly diagnosed lung cancer patients is as high as 85%. Despite improvements in the diagnosis and treatment of lung cancer over the past decade, the overall 5-year patient survival rate remains below 16%. Statistics released by the China Cancer Center show that among the 4.29 million new cancer patients, lung cancer accounts for 733,000; among the 2.8 million cancer deaths, lung cancer accounts for 610,000 of them, making it the veritable "first cancer" in my country. Among them, about 75% of the patients are already in the middle and advanc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F13/00A61K51/04A61K103/10
CPCA61K51/0459C07B2200/05C07F13/005
Inventor 李芳巍董祥梅徐建忠刘晓冬张琦李强梁爽
Owner MUDANJIANG MEDICAL UNIV
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