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Compound for treating stomach cancer, and preparation method and use thereof

A compound and technology for the treatment of liver cancer, applied in rhodium organic compounds, platinum group organic compounds, chemical instruments and methods, etc., can solve problems such as difficulties, side effects and complicated clinical application, and achieve the effect of low cost, molecular stability, and good selectivity

Inactive Publication Date: 2018-12-18
GUANGXI UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the frequent occurrence of serious side effects and drug resistance make clinical application complicated and difficult
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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  • Compound for treating stomach cancer, and preparation method and use thereof
  • Compound for treating stomach cancer, and preparation method and use thereof
  • Compound for treating stomach cancer, and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The compound for treating gastric cancer is prepared by a one-pot method.

[0027] The one-pot method specifically includes the following steps: Weigh 170 mg of 2-(4-pyridyl) benzimidazole, add 15 mL of carbon tetrachloride solvent, 5 mg of p-toluenesulfonic acid monohydrate, and 172 mg of N-bromobutane imide, heated to 65 ° C for 20 h, and the solvent was removed by rotary evaporation, and then 115 mg of 7-bromoindazole and 26.5 to 36.5 mg of dichloro(pentamethylcyclopentadienyl) rhodium (III) were added, and then Dissolve together in 10mL of anhydrous toluene, add 0.05mL of ethylenediamine dropwise while stirring, then add 1mg of cesium carbonate, 4mL of triethylamine, then pass nitrogen gas for 30min, add 10mg of tetrakis(triphenylphosphine) Palladium, 1.4 mg of CuI, 45 mg of propynyl p-toluenesulfonate, heated to 70°C for 22 hours, then added hydrochloric acid dropwise until the solution became neutral, and an orange solid was precipitated, which was the compound fo...

Embodiment 2

[0029] The compound for treating gastric cancer is prepared by a one-pot method. The one-pot method specifically includes the following steps: Weigh 175 mg of 2-(4-pyridyl)benzimidazole, add 20 mL of carbon tetrachloride solvent, 10 mg of p-toluenesulfonic acid monohydrate, and 177 mg of N-bromosuccinyl Amine, heated to 70 ° C for 24 hours, rotary evaporation to remove the solvent, then added 120 mg of 7-bromoindazole, 31.5 mg of dichloro (pentamethylcyclopentadienyl) rhodium (III), and then dissolved in 15 mL of Water toluene, add 0.1mL ethylenediamine dropwise while stirring, then add 3mg cesium carbonate, 6mL triethylamine, then pass through nitrogen for 30min, add 15mg tetrakis (triphenylphosphine) palladium, 1.9mg CuI, 50mg p-toluene After propynyl sulfonate was heated to 80°C for 24 hours, hydrochloric acid was added dropwise until the solution became neutral, and an orange solid was precipitated, which was the compound for treating gastric cancer. This compound is a rh...

Embodiment 3

[0032] The compound for treating gastric cancer is prepared by a one-pot method.

[0033] The one-pot method specifically includes the following steps: Weigh 180 mg of 2-(4-pyridyl)benzimidazole, add 25 mL of carbon tetrachloride solvent, 15 mg of p-toluenesulfonic acid monohydrate, and 182 mg of N-bromobutane imide, heated to 75 ° C for 26 hours, and the solvent was removed by rotary evaporation, and then 125 mg of 7-bromoindazole and 26.5 mg of dichloro(pentamethylcyclopentadienyl) rhodium (III) were added, and then dissolved together In 20mL of anhydrous toluene, add 0.15mL of ethylenediamine dropwise while stirring, then add 5mg of cesium carbonate, 8mL of triethylamine, then pass nitrogen gas for 30min, add 20mg of tetrakis(triphenylphosphine) palladium, 2.4 mg of CuI and 55 mg of propynyl p-toluenesulfonate were heated to 90°C for 26 hours, then hydrochloric acid was added dropwise until the solution became neutral, and an orange solid was precipitated, which was the com...

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Abstract

The invention discloses a compound for treating gastric cancer. The chemical structural formula of the compound is shown in the description. The invention also discloses a preparation method and a useof the compound for treating gastric cancer. The compound for treating gastric cancer contains a benzimidazole and indazole heterocyclic ring, so the obtained compound for treating gastric cancer hasa good bioactivity; and the compound has a large conjugated system, so the molecule is stable. The preparation method has the advantages of simplicity, low cost, no separation or purification steps in the reaction process, reduction of the loss of raw materials, and meeting the requirements of green chemistry.

Description

technical field [0001] The invention relates to the technical field of compound preparation, in particular to a compound for treating gastric cancer and its preparation method and application. Background technique [0002] Cancer and malignancy are difficult-to-treat diseases characterized by high lethality. Despite tremendous efforts by scientific researchers to improve treatment, existing drugs have a relatively limited effective range of action, and there is a considerable need to develop new drugs and alternative therapies. Platinum antineoplastic drugs (such as cisplatin, carboplatin or oxaliplatin) are the most used at present, which have a significant impact on current tumor chemotherapy. However, severe side effects and frequent occurrence of drug resistance make clinical application complicated and difficult. 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 tum...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61K31/555A61P35/00A61P29/00
CPCC07F15/008A61P29/00A61P35/00
Inventor 李培源霍丽妮
Owner GUANGXI UNIV OF CHINESE MEDICINE
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