Benzimidazole pyridine complex and method for preparing same

A technology of benzimidazopyridines and benzimidazopyridines, applied in the field of anticancer compounds, can solve the problems of large toxic and side effects, long course of treatment, high toxicity and the like, and achieves simple and feasible method, strong antitumor activity and good stability Effect

Inactive Publication Date: 2013-03-13
YULIN NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The current clinical treatment of tumors includes surgery, radiotherapy, and chemotherapy. Most of the drugs currently used for treatment are chemical drugs. Although they can relieve symptoms and prolong the course of the disease, there are still many problems: especially because chemotherapy drugs are highly toxic Tumor cells also damage the body's own immune cells such as white blood cells and lymphocytes, resulting in patients often being infected concurrently

Method used

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  • Benzimidazole pyridine complex and method for preparing same
  • Benzimidazole pyridine complex and method for preparing same
  • Benzimidazole pyridine complex and method for preparing same

Examples

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Embodiment 1

[0050] One, preparation method of the present invention:

[0051] (1) Preparation of 2,6-dibenzimidazolpyridine: Weigh 3.35 g of 2,6-dicarboxylic acid pyridine (20 mmol) and 0.476 g of o-phenylenediamine (44 mmol) as reactants, and use 50 mL of polymer Phosphoric acid is used as a solvent, and after being fully mixed, put it into a microwave rapid reaction system, and react at a power of 200w and a temperature of 100°C for 2 minutes; After the green reaction solution was cooled to room temperature, it was poured into 100 mL of ice water, and it turned into a pink turbid solution. It was neutralized with NaOH to pH=9~10, and a pink precipitate was produced. It was suction filtered once, and washed 3 times with distilled water to obtain the crude product. The crude product was recrystallized with methanol, filtered once with suction, washed with distilled water for 3 times, placed in a drying oven at 80°C, and baked for 20-30 minutes to obtain a white columnar compound which is...

Embodiment 2

[0072] One, preparation method of the present invention:

[0073] (1) Preparation of 2,6-dibenzimidazolpyridine: Weigh 3.35 g of 2,6-dicarboxylic acid pyridine (20 mmol) and 0.476 g of o-phenylenediamine (60 mmol) as reactants, and use 70 mL of polymer Phosphoric acid is used as a solvent. After fully mixing evenly, put it into a microwave rapid reaction system, and react at a power of 250w and a temperature of 110°C for 3 minutes; then react at a power of 350w and a temperature of 100°C for 5 minutes. After the green reaction solution was cooled to room temperature, it was poured into 100mL of ice water, and it turned into a pink turbid solution. It was neutralized with NaOH to pH=9~10, and a pink precipitate was produced. It was suction filtered once, washed twice with distilled water, and the obtained crude product. Recrystallize the crude product with methanol, filter it once with suction, wash it twice with distilled water, put it in a drying oven at 90°C, and bake it fo...

Embodiment 3

[0095] One, preparation method of the present invention:

[0096] (1) Preparation of 2,6-dibenzimidazolpyridine: Weigh 3.35 g of 2,6-dicarboxylic acid pyridine (20 mmol) and 0.476 g of o-phenylenediamine (40 mmol) as reactants, and use 50 mL of polymer Phosphoric acid is used as a solvent, and after being fully mixed, put it into a microwave rapid reaction system and react for 2 minutes at a power of 220w and a temperature of 80°C; then react for 7 minutes at a power of 320w and a temperature of 120°C. After the green reaction solution was cooled to room temperature, it was poured into 100mL of ice water, and it turned into a pink turbid solution. It was neutralized with NaOH to pH=9~10, and a pink precipitate was produced. It was suction filtered once, washed twice with distilled water, and the obtained crude product. Recrystallize the crude product with methanol, filter it with suction once, wash it twice with distilled water, put it in a drying oven at 80°C, and bake it fo...

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Abstract

The invention discloses a benzimidazole pyridine complex and a method for preparing the same. The method is that Pb(NO3)2, 2, 6-bisbenzimidazole pyridine (bbp) and 5-nitroisophthalicacid (nipa) are proportionally weighed according to the molar ratio of 1:1:(1-0.5) to be put into a container and are added with water to be stirred for 10-15 minutes; then, the stirred raw material liquid is poured into a reactor, the reactor is covered to be heated to 160-165 DEG C, and then, thermal insulation reaction is carried out for 115-120 hours; and a gradient heating method is adopted to cool the raw material liquid to room temperature so as to obtain a colorless blocky crystal complex, i.e. the benzimidazole pyridine complex [Pb2(nipa) (Hbbp)2]n.nH2O is obtained. The benzimidazole pyridine complex has the characteristics of good stability and obvious functions in inhibiting three types of human cancer cells of human breast cancer cells, lung cancer cells and cervical cancer cells, and provides guidance for the research and development of an anticancer complex.

Description

technical field [0001] The invention belongs to anticancer compounds, in particular to a benzimidazolpyridine complex and a preparation method thereof, and its application as an antitumor compound. Background technique [0002] Malignant tumors are a large class of diseases that seriously threaten human health. Their abnormal proliferation is controlled by abnormal information in cells and is closely related to the abnormal activity and inactivation of corresponding genes in tumor cells. Common malignant tumors in my country include: lung cancer, gastric cancer, esophageal cancer, colon cancer, liver cancer, cervical cancer, breast cancer, leukemia, malignant lymphoma, nasopharyngeal cancer and other ten tumors. Among them, lung cancer, gastric cancer, esophageal cancer, liver cancer, breast cancer, and cervical cancer are the most common, accounting for about 70% to 80% of all malignant tumors. [0003] The current clinical treatment of tumors includes surgery, radiotherap...

Claims

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Application Information

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IPC IPC(8): C07F7/24A61K31/555A61P35/00
Inventor 杨燕罗旭健颜六廷
Owner YULIN NORMAL UNIVERSITY
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