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Drug for treating malignant tumors

A malignant tumor and drug technology, applied in the direction of antineoplastic drugs, drug combinations, antibacterial drugs, etc., can solve the problems of limited application and achieve the effect of enriching the library of therapeutic compounds

Inactive Publication Date: 2017-08-11
徐晓东
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Vancomycin is the drug of choice for the treatment of MRSA infection, but its adverse drug reactions limit its clinical application

Method used

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  • Drug for treating malignant tumors
  • Drug for treating malignant tumors
  • Drug for treating malignant tumors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Synthesis of 2-thiazolylmethyl-4-phenyl-7-fluoro-quinoxalinyl-6-secondary amine

[0035] The synthetic route is:

[0036]

[0037] Synthetic steps:

[0038] 1-1 Synthesis of 4-chloro-7-fluoro-quinazolinyl-6-amine

[0039]

[0040] Add 40 ml of methanol and tetrahydrofuran (3:1 by volume) to 4-chloro-7-fluoro-6-nitro-quinazoline (10 mmol), stir for 20 minutes, dissolve completely, and then cool down to 0-5°C, add 1 g of sodium borohydride to it, keep the temperature and stir for two hours, then rise to room temperature and continue to stir for 4 hours, add 40 ml of water to the reaction, extract with 50 ml of ethyl acetate, and use anhydrous Dry over sodium sulfate for 2 hours, filter, evaporate the organic solvent to dryness, and dry under vacuum at 50°C to obtain 1.8 g of a yellow solid, which is 4-chloro-7-fluoro-quinazolinyl-6-amine, with a yield of 91%. 1 H-NMR (400 MHz, CDCl 3 ) δ: 6.94(m,2H), 7.04(s,2H), 9.56(s,1H). 13 C-NMR (75 MHz, CDCl 3 ...

Embodiment 2

[0050] Example 2: Synthesis of 2-thiazolylmethyl-4-(2-naphthyl)-7-fluoro-quinoxalinyl-6-secondary amine

[0051]

[0052] The synthesis method is as 1-4 in Example 1, and 2-thiazolylmethyl-4-chloro-7-fluoro-quinoxalinyl-6-secondary amine (10 mmol) is dissolved in 30 ml of nitrogen-nitrogen dimethylformamide During the process, the system was blown with argon for 20 minutes, and the air in the system was evacuated, then tetrakistriphenylphosphine palladium was added, the temperature was raised to 60°C, and stirring was continued for half an hour, 2-naphthylboronic acid (12 mmol) was added thereto, and then 10 milliliters of sodium carbonate (1 gram) aqueous solution was warmed up to 90° C., stirred for 5 hours, kept feeding argon during the whole process, then lowered the temperature, evaporated the solvent under reduced pressure, and the solid passed through the chromatographic column quickly.

[0053] 3.4 g of off-white 2-thiazolylmethyl-4-(2-naphtenyl)-7-fluoro-quinoxalin...

Embodiment 3

[0054] Example 3: Synthesis of 4-[7-fluoro-6-(2-thiazolylmethylamino)]quinoxalinyl-benzonitrile

[0055]

[0056] The synthesis method is as 1-4 in Example 1, and 2-thiazolylmethyl-4-chloro-7-fluoro-quinoxalinyl-6-secondary amine (10 mmol) is dissolved in 30 ml of nitrogen-nitrogen dimethylformamide In the system, the system was blown with argon for 20 minutes, and the air in the system was evacuated, then tetrakistriphenylphosphine palladium was added, the temperature was raised to 60°C, and stirring was continued for half an hour, p-cyanophenylboronic acid (12 mmol) was added thereto, and then Add 10 milliliters of sodium carbonate (1 gram) aqueous solution, raise the temperature to 90° C., stir for 5 hours, keep feeding argon during the whole process, then lower the temperature, evaporate the solvent under reduced pressure, and the solid quickly passes through the chromatographic column to obtain 3.3 grams of light yellow 4- [7-Fluoro-6-(2-thiazolylmethylamino)]quinoxali...

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Abstract

The invention discloses a drug for treating malignant tumors, and the chemical structural formula is a formula (II). Malignant tumors are lung cancer, liver cancer, neurogliocytoma, adenocarcinoma of ovary, breast cancer or chronic myelogenous leukemia. The drug disclosed by the invention enriches a malignant tumor treatment compound library and plays a positive role on treatment of cancer.

Description

technical field [0001] The invention relates to a medicine for treating malignant tumors. Background technique [0002] Cancer is a malignant disease with a very high mortality rate. It is difficult to treat and has a high mortality rate, which brings a heavy burden to patients and families. In recent years, the incidence of cancer in our country has increased significantly, making cancer prevention and treatment face a severe situation. In recent years, the incidence of cancer in my country has gradually increased, which has attracted widespread attention from people from all walks of life. According to relevant research reports, in the 1970s, cancer in my country increased from 10.13% to 22.32%, and the death rate increased by 82.11%. Cancer is the number one cause of death in cities and the second in rural areas. Especially in today's aging population, smoking, dietary changes, microbial infections, obesity, reduced activity, poor work and rest, and other factors are t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/12A61K31/517A61P35/00A61P35/02A61P31/04
CPCA61P31/04A61P35/00C07D417/12
Inventor 曹艳
Owner 徐晓东
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