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A kind of fluorophenyl ruthenium compound and its preparation method and application

A kind of fluorobenzene ruthenium compound and ruthenium compound technology are applied in the field of ruthenium compound preparation, and achieve the effects of strong inhibitory activity, low cost and easy availability of raw materials

Inactive Publication Date: 2017-12-05
THE SIXTH CONSTR CO LTD OF CHINA NAT CHEM ENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, dozens of anti-tumor drugs currently used in clinical chemotherapy or adjuvant therapy only have a good curative effect on the treatment of some tumors

Method used

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  • A kind of fluorophenyl ruthenium compound and its preparation method and application
  • A kind of fluorophenyl ruthenium compound and its preparation method and application
  • A kind of fluorophenyl ruthenium compound and its preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0026] A fluorophenyl ruthenium compound, said fluorophenyl ruthenium compound has the structure of (I):

[0027]

[0028] A preparation method of fluorophenyl ruthenium compound, comprising the following steps:

[0029] Step 1. Dissolve 1g of ruthenium trichloride hydrate and 30mL of γ-terpinene in 70mL of absolute ethanol, heat and reflux and stir for 6 hours, and leave to precipitate to obtain dichloro-dichloro-di-methylisopropyl Benzodiruthenium;

[0030] Step 2. Weigh 8g of diflunisalate and dissolve it in 40mL of solvent, add 4g of N,N-dimethylformamide as a catalyst, then add substituted phenylacetyl chloride, react at 65°C for 8 hours, remove After solvent, obtain phenylacetyl fluorophenyl salicylic acid;

[0031] Step 3. Dissolve 1 g of dichloro-di-methylcymene diruthenium dichloride and 3 g of phenylacetylfluorophenylsalicylic acid in 80 mL of tetrahydrofuran, react at 65° C. for 6 hours, and purify. Instantly.

[0032] Wherein, the ruthenium trichloride hydra...

Embodiment 2

[0037] A preparation method of fluorophenyl ruthenium compound, comprising the following steps:

[0038] Step 1. Dissolve 6g of ruthenium trichloride hydrate and 80mL of γ-terpinene in 200mL of absolute ethanol, heat and reflux and stir for 6 hours, and leave to precipitate to obtain dichloro-dichloro-di-methylisopropyl Benzodiruthenium.

[0039] Step 2: Weigh 12g of diflunisalate and dissolve it in 80mL of solvent, add 8g of N,N-dimethylformamide as a catalyst, then add substituted phenylacetyl chloride, react at 75°C for 12 hours, remove After solvent, phenylacetylfluorophenylsalicylic acid is obtained.

[0040] Step 3. Dissolve 3 g of dichloro-di-methylcymene diruthenium dichloride and 9 g of phenylacetylfluorophenylsalicylic acid in 100 mL of tetrahydrofuran, react at 75° C. for 10 hours, and purify. Instantly.

[0041] Wherein, the ruthenium trichloride hydrate in the step 1 is ruthenium trichloride hydrate with a ruthenium weight content of 45%; the purity of the γ-te...

Embodiment 3

[0046] A preparation method of fluorophenyl ruthenium compound, comprising the following steps:

[0047] Step 1. Dissolve 3g of ruthenium trichloride hydrate and 60mL of γ-terpinene in 120mL of absolute ethanol, heat and reflux and stir for 6 hours, and leave to precipitate to obtain dichloro-dichloro-di-methylisopropyl Benzodiruthenium;

[0048] Step 2. Weigh 10 g of diflunisalate and dissolve it in 60 mL of solvent, add 6 g of N,N-dimethylformamide as a catalyst, then add substituted phenylacetyl chloride, react at 70 ° C for 10 hours, remove After solvent, obtain phenylacetyl fluorophenyl salicylic acid;

[0049] Step 3. Dissolve 2 g of dichloro-di-methylcymene diruthenium dichloride and 6 g of phenylacetylfluorophenylsalicylic acid in 90 mL of tetrahydrofuran, react at 70° C. for 8 hours, and purify. Instantly.

[0050] Wherein, the ruthenium trichloride hydrate in the step 1 is ruthenium trichloride hydrate with a ruthenium weight content of 45%; the purity of the γ-terp...

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Abstract

The present invention provides a fluorine benzene ruthenium compound and a preparation method and application thereof. The structure of the fluorine benzene ruthenium compound is shown in formula (I). The fluorine benzene ruthenium compound is synthesized and generated by dichloridized dichloro-2-methyl-isopropyl-benzo dirhodium and phenylacetyl diflunisal and shows a relatively strong inhibition activity on a human lymph cancer cell strain and a liver cancer strain of a human body. The fluorine benzene ruthenium compound can be used for preparing medicines for treating liver cancer and lymph cancer, and can be prepared to injections, tablets, pellets, capsules, suspensions or emulsions. The fluorine benzene ruthenium compound provided by the invention can improve the lipid solubility and the permeability of medicines, enhances the dissolubility of a biological film and prompts the speed of absorption and transmission in vivo, so that the physiological action changes.

Description

technical field [0001] The invention relates to the field of preparation of ruthenium compounds, more specifically, the invention relates to a fluorophenyl ruthenium compound and its preparation method and application. Background technique [0002] Liver cancer refers to malignant tumors that occur in the liver, including primary liver cancer and metastatic liver cancer. People usually refer to primary liver cancer when they say liver cancer. Primary liver cancer is one of the most common malignant tumors in clinical practice. According to the latest statistics, there are about 600,000 new liver cancer patients in the world every year, ranking fifth among malignant tumors. According to cell type, primary liver cancer can be divided into hepatocellular carcinoma, cholangiocellular carcinoma and mixed liver carcinoma. [0003] Possible causes of lymphoma include a lack of immune system, viral infection, use of radiation or drugs, and genetics. Studies have pointed out that t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F15/00A61K31/28A61K31/616A61P35/00
CPCC07F15/0053
Inventor 曹满英
Owner THE SIXTH CONSTR CO LTD OF CHINA NAT CHEM ENG
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