Substituted diaryl compound and preparation method and antiviral application thereof
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A compound, aryl technology, applied in the field of preparation of said compound
Active Publication Date: 2011-10-05
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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The compounds of the present invention and their effects have not been reported so far in relevant literature both at home and abroad.
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Embodiment 1
[0109] Synthesis of (3-propionylamino-4-methoxyphenyl)formyl (3',4',5'-trimethoxyphenyl)amine (1)
[0110] In a 25ml flask, after dissolving 3-amino-4-methoxybenzoic acid (1.0g, 6mmol) in dry THF (tetrahydrofuran), triethylamine (1.2ml, 12mmol) was added to obtain a yellow transparent solution, nitrogen Protected, stirred, and propionyl chloride (0.78ml, 9mmol) was added dropwise thereto under ice-water bath conditions, and the reaction at room temperature was naturally restored after the dropwise addition was completed. The reaction solution was filtered, and the filtrate was evaporated to dryness and separated on a silica gel column to obtain 1.3 g of 3-propionylamino-4-methoxybenzoic acid (yield 67%).
[0111] Mix 100mg (0.45mmol) of the above product with 136mg (0.6mmol) of HOBT and 0.1ml (0.8mmol) of DIC in dry DMF under ice-water bath conditions, N 2 protection, after stirring for 30 min, 72 mg (mmol) of 3,4,5-trimethoxyaniline was added, and the mixture was naturally...
Embodiment 2
[0112] Synthesis of (3-propionylamino-4-methoxyphenyl)formyl (4'-chlorophenyl)amine (2)
[0113] Using 3-amino-4-methoxybenzoic acid, propionyl chloride and p-chloroaniline as starting materials, according to the method similar to Example 1, compound 2 was synthesized with a yield of 23%. 1 See Table 1 for H NMR data.
Embodiment 3
[0114] Synthesis of (3-trifluoroacetamido-4-methoxyphenyl)formyl (4'-chlorophenyl)amine (4)
[0115] Using 3-amino-4-methoxybenzoic acid, trifluoroacetic anhydride and p-chloroaniline as starting materials, according to the method similar to Example 1, compound 4 was synthesized with a yield of 26%. 1 See Table 1 for H NMR data.
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Abstract
The invention provides substituted diaryl compounds as shown in general formula (I) or their pharmaceutically acceptable salts, and also provides a preparation method; a class of novel broad-spectrum antiviral compounds and pharmaceutical salts targeting cytokines are screened and obtained through studies on structure-activity relationship and action mechanism of active compounds; the compounds not only have significant broad-spectrum antiviral activity, but also have the advantages of low toxicity and good pharmaceutical properties.
Description
technical field [0001] The present invention relates to a group of substituted biaryl compounds, and also relates to the preparation method of the compounds and the application in broad-spectrum anti-virus, especially anti-hepatitis virus, anti-respiratory virus, enterovirus and anti-AIDS virus. Background technique [0002] At present, the antiviral drugs used clinically all target viral proteins, and the mechanism of action is to inhibit the replication of the virus or block the invasion of the virus. Viruses are "moving targets" that rely on continuous mutation to evade drug attacks. Drugs targeting viral proteins all cause virus mutation and drug resistance, which has become a worldwide problem. Similarly, except for interferon, the six drugs currently clinically used for the treatment of hepatitis B are all nucleoside analogues, and their targets are all viral protein DNA polymerases. After long-term use, severe drug resistance will occur. problems, leading to treatme...
Claims
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