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Fluorine benzene ruthenium compound and preparation method and application thereof

A fluorobenzene ruthenium compound and a ruthenium compound technology are applied in the field of ruthenium compound preparation, and achieve the effects of easy availability of raw materials, simple preparation method and strong inhibitory activity

Inactive Publication Date: 2015-08-19
THE SIXTH CONSTR CO LTD OF CHINA NAT CHEM ENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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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  • Fluorine benzene ruthenium compound and preparation method and application thereof
  • Fluorine benzene ruthenium compound and preparation method and application thereof
  • Fluorine benzene ruthenium compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] A fluorobenzeneruthenium compound, the fluorobenzeneruthenium compound has the structure of (I):

[0027]

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

[0029] Step 1. Dissolve 1 g of hydrated ruthenium trichloride and 30 mL of γ-terpinene in 70 mL of dehydrated ethanol, heat under reflux for 6 hours, and stand to separate out to obtain dichloro-di-methylisopropyl dichloride. diruthenium benzene;

[0030] Step 2: Weigh 8g of difluorobenzenesalicylic acid 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 the solvent, phenylacetyl fluorobenzene salicylic acid is obtained;

[0031] Step 3. Dissolve 1g of dichloro-di-methylisopropylbenzenediruthenium dichloride and 3g of phenylacetylfluorobenzenesalicylic acid in 80mL of tetrahydrofuran, react at 65°C for 6 hours, and purify, That's it.

[0032] W...

Embodiment 2

[0037] A preparation method of a fluorobenzene ruthenium compound, comprising the following steps:.

[0038] Step 1. Dissolve 6g of hydrated ruthenium trichloride and 80mL of γ-terpinene in 200mL of dehydrated ethanol, heat under reflux for 6 hours, and stand to separate out to obtain dichloro-di-methylisopropyl dichloride. diruthenium benzene.

[0039] Step 2: Weigh 12g of difluorobenzenesalicylic acid 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, phenylacetylfluorobenzenesalicylic acid is obtained.

[0040] Step 3. Dissolve 3g of dichloro-di-methylisopropylbenzene diruthenium dichloride and 9g of phenylacetylfluorobenzenesalicylic acid in 100mL of tetrahydrofuran, react at 75°C for 10 hours, and purify, That's it.

[0041] Wherein, the hydrated ruthenium trichloride in the first step is hydrated ruthenium trichloride with a ruthenium weight co...

Embodiment 3

[0046] A preparation method of a fluorobenzene ruthenium compound, comprising the following steps:.

[0047] Step 1. Dissolve 3g of hydrated ruthenium trichloride and 60mL of γ-terpinene in 120mL of absolute ethanol, heat under reflux for 6 hours, and stand to separate out to obtain dichloro-di-methylisopropyl dichloride. diruthenium benzene;

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

[0049] Step 3. Dissolve 2g of dichloro-di-methylisopropylbenzenediruthenium dichloride and 6g of phenylacetylfluorobenzenesalicylic acid in 90mL of tetrahydrofuran, react at 70°C for 8 hours, and purify, That's it.

[0050] Wherein, the hydrated ruthenium trichloride in the first step is hydrated ruthenium trichloride with a ruthenium weight con...

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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 present invention relates to the field of preparation of a ruthenium compound, more particularly, the present invention relates to a ruthenium fluorobenzene compound and a preparation method and application thereof. Background technique [0002] Liver cancer refers to malignant tumors that occur in the liver, including primary liver cancer and metastatic liver cancer. People often say liver cancer refers to primary liver cancer. Primary liver cancer is one of the most common malignant tumors in clinic. According to the latest statistics, there are about 600,000 new liver cancer patients in the world every year, ranking fifth among malignant tumors. Primary liver cancer can be divided into hepatocellular carcinoma, cholangiocarcinoma and mixed hepatocellular carcinoma according to cell type. [0003] Possible causes of lymphoma include a deficiency of the immune system, viral infection, use of radiation or drugs, and genetics. Studies have shown t...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61K31/28A61K31/616A61P35/00
CPCC07F15/0053
Inventor 张浩肖晓阳
Owner THE SIXTH CONSTR CO LTD OF CHINA NAT CHEM ENG
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