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Use of a class of n-alkylindole compounds in the preparation of anti-influenza virus drugs

A technology of influenza virus and compound, applied in the field of medicine, can solve the problems of undiscovered anti-HIV and anti-influenza virus activity

Active Publication Date: 2020-03-31
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] In addition, there are also reports in the literature that the nitrogen atom of indole is an alkyl-substituted complex structure derivative [39] , but they were not found to have anti-HIV and anti-influenza virus activity

Method used

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  • Use of a class of n-alkylindole compounds in the preparation of anti-influenza virus drugs
  • Use of a class of n-alkylindole compounds in the preparation of anti-influenza virus drugs
  • Use of a class of n-alkylindole compounds in the preparation of anti-influenza virus drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0191] Embodiment 1: the preparation of methyl 2-[2-(1-ethyl-1H-indol-3-yl)acetamido]benzoate

[0192]

[0193] The first step, weigh indole acetic acid (1.05g), add DMF (5mL) and stir to dissolve, cool down to 0-5°C and stir; add 60% sodium hydride (0.72g), stir for 10min, add bromoethane (0.98 g), react at 0-5°C for 0.5h, slowly rise to room temperature and react for 2h; add ethyl acetate (40mL), water (40mL); stir rapidly, add 10mL of 6N hydrochloric acid solution dropwise within 2mim, stir for 5min; separate phases, water The phases were extracted with ethyl acetate (20 mL), and the phases were separated, and the ethyl acetate phases were combined; saturated brine (30 mL) was added to stir rapidly for 5 min, and the phases were separated, and the ethyl acetate phase was removed under reduced pressure at 50 ° C to obtain the crude product of the first step 2 -(1-Ethyl-1H-indol-3-yl)acetic acid.

[0194] In the second step, the first step product 2-(1-ethyl-1H-indol-3-yl...

Embodiment 2

[0195] Embodiment 2: Preparation of methyl 2-[2-(1-propyl-1H-indol-3-yl)acetamido]benzoate

[0196]

[0197] The first step, weigh indole acetic acid (1.05g), add DMF (5mL) and stir to dissolve, cool down to 0-5°C and stir; add 60% sodium hydride (0.72g), stir for 10min, add bromopropane (1.1g ), react at 0-5°C for 0.5h, slowly rise to room temperature and react for 2h; add ethyl acetate (40mL), water (40mL); stir rapidly, add 10mL of 6N hydrochloric acid solution dropwise within 2mim, stir for 5min; separate phase, water phase Extract with ethyl acetate (20mL), separate the phases, and combine the ethyl acetate phases; add saturated brine (30mL) and stir rapidly for 5min, separate the phases, remove the solvent from the ethyl acetate phase at 50°C under reduced pressure to obtain the crude product of the first step 2- (1-Propyl-1H-indol-3-yl)acetic acid.

[0198] In the second step, the first step product 2-(1-propyl-1H-indol-3-yl)acetic acid was added into dichloromethan...

Embodiment 3

[0199] Example 3: Preparation of N-(3-chloropyridin-4-yl)-2-(1-ethyl-1H-indol-3-yl)acetamide

[0200]

[0201] The first step, weigh indole acetic acid (1.05g), add DMF (5mL) and stir to dissolve, cool down to 0-5°C and stir; add 60% sodium hydride (0.72g), stir for 10min, add bromoethane (0.98 g), react at 0-5°C for 0.5h, slowly rise to room temperature and react for 2h; add ethyl acetate (40mL), water (40mL); stir rapidly, add 10mL of 6N hydrochloric acid solution dropwise within 2min, stir for 5min; separate phases, water The phases were extracted with ethyl acetate (20 mL), and the phases were separated, and the ethyl acetate phases were combined; saturated brine (30 mL) was added to stir rapidly for 5 min, and the phases were separated, and the ethyl acetate phase was removed under reduced pressure at 50 ° C to obtain the crude product of the first step 2 -(1-Ethyl-1H-indol-3-yl)acetic acid.

[0202] In the second step, the first step product 2-(1-ethyl-1H-indol-3-yl)...

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Abstract

The invention discloses an application of indole compounds represented by general formula (I), and derivatives and pharmaceutically acceptable salts thereof in the preparation of anti-influenza virus medicines or healthcare products, and also discloses a preparation method of the compounds, and an application of medicinal compositions containing the compounds in the preparation of the anti-influenza virus medicines or healthcare products.

Description

technical field [0001] The present invention relates to an indole derivative and its pharmaceutically acceptable salt, their preparation method, a pharmaceutical composition containing this type of compound, and the application of this type of compound in anti-HIV virus and anti-influenza virus, belonging to field of medical technology. Background technique [0002] Human Immunodeficiency Virus (Human Immunodeficiency Virus, HIV) infects human immune cells and destroys the human immune system, causing patients to eventually die of complications such as severe infection or secondary tumors. The disease caused by the virus is called Acquired Immunodeficiency Syndrome, or AIDS [1] . [0003] According to the report of the United Nations Program on AIDS (UNAIDS), by the end of 2012, the number of HIV-infected people in the world was 35 million [32.2 million-38.8 million], including 3.3 million children [3 million-3.7 million]. In 2012, there were 2.3 million [1.9 million-2.7 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D209/18C07D401/12A61K31/4015A61K31/4439A61P31/16
CPCC07D209/18C07D401/12
Inventor 石建功郭颖徐成博陈勍陈明华霸明宇朱承根唐克蒋建东郭家梅郭庆兰林生杨永春
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI