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Synthesis of a kind of aniline sulfonyl compound and its application as HIV virus inhibitor

A compound, composition technology, applied in the field of biochemistry

Active Publication Date: 2018-05-29
UNIV OF SCI & TECH OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, there are no drugs and therapies that can effectively treat AIDS in the world, and only drugs can be used to properly control the proliferation of HIV in the human body

Method used

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  • Synthesis of a kind of aniline sulfonyl compound and its application as HIV virus inhibitor
  • Synthesis of a kind of aniline sulfonyl compound and its application as HIV virus inhibitor
  • Synthesis of a kind of aniline sulfonyl compound and its application as HIV virus inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] 1, prepare the compound shown in formula I of the present invention (R 1 for -H,R 2 for -H,R 3 for -(CH 2 ) 3 -CH 3 ,R 4 for -H,R 5 for -H,R 6 for-Ph, R 7-Ph, X is O, n is 2) the name is 3-(N-(4-butylphenyl)phenylsulfonamido)propyl benzenesulfonate. 3mmol 4-butylaniline, 6mmol 3-chloropropanol and 3mmol sodium ethylate were refluxed in 20mL ethanol for 8 hours, and column chromatography was separated to obtain 3-((4-butylphenyl)amino)propan-1-alcohol; 1mmol 3 -((4-butylphenyl)amino)propan-1-alcohol and 2mmol of triethylamine are dissolved in methylene chloride, cooled in an ice bath, 2mmol of benzenesulfonyl chloride is added dropwise to the above solution, and after the addition is completed, transfer to React at room temperature for 10-15 hours. Then column chromatography separated to obtain 3-(N-(4-butylphenyl)phenylsulfonamido)propyl benzenesulfonate.

[0073] The reaction formula is as follows:

[0074]

[0075] The compound prepared 1 H nuclear mag...

Embodiment 2

[0086] 1, prepare the compound shown in formula I of the present invention (R 1 for -H,R 2 for -H,R 3 for -(CH 2 ) 3 -CH 3 ,R 4 for -H,R 5 for -H,R 6 for -Ph- t Bu(p), R 7 for -Ph- t Bu(p), X is O, n is 1) name is 4-(tert-butyl)benzenesulfonic acid 2-(4-(tert-butyl)-N-(4-butylphenyl)phenylsulfonamide base) ethyl ester.

[0087] 3mmol of formula 4-butylaniline, 6mmol of 2-chloroethanol and 3mmol of sodium ethylate were refluxed in 20mL of ethanol for 8 hours, separated by column chromatography to obtain 2-((4-butylphenyl)amino)ethanol; 1mmol of 2-(( Dissolve 4-butylphenyl)amino)ethanol and 1 mmol of triethylamine in dichloromethane, cool in an ice bath, add 2 mmol of 4-tert-butylbenzenesulfonyl chloride dropwise to the above solution, and transfer to room temperature after the addition is complete React for 10 to 15 hours. Then column chromatography separated to obtain 2-(4-(tert-butyl)-N-(4-butylphenyl)phenylsulfonamido)ethyl 4-(tert-butyl)benzenesulfonate.

[00...

Embodiment 3

[0095] 1, prepare the compound shown in formula I of the present invention (R 1 for -H,R 2 for -H,R 3 for -(CH 2 ) 3 -CH 3 ,R 4 for -H,R 5 for -H,R 6 for-Ph-CH 3 (p), R 7 for-Ph-CH 3 (p), X is O, n is 1) the name is 2-(N-(4-butylphenyl)-4-methylphenylsulfonamido)ethyl 4-methylbenzenesulfonate.

[0096] 3mmol of formula 4-butylaniline, 6mmol of 2-chloroethanol and 3mmol of sodium ethylate were refluxed in 20mL of ethanol for 8 hours, separated by column chromatography to obtain 2-((4-butylphenyl)amino)ethanol; 1mmol of 2-(( Dissolve 4-butylphenyl)amino)ethanol and 1mmol of triethylamine in dichloromethane, cool in an ice bath, add 2mmol of 4-methylbenzenesulfonyl chloride dropwise to the above solution, and transfer to room temperature for reaction 10-15 hours. Then column chromatography separated 2-(N-(4-butylphenyl)-4-methylphenylsulfonamido)ethyl 4-methylbenzenesulfonate.

[0097] The reaction formula is as follows:

[0098]

[0099] The compound prepared 1...

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PUM

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Abstract

The invention discloses a compound and its preparation method and application. The compound of formula I has a structure shown in the present invention. The compound of formula I of the present invention targets the host's own conserved cellular protein PCAF BRD, and has the potential to solve the drug resistance problem caused by the high mutation of HIV virus, and has better It has the activity of inhibiting the proliferation of HIV virus and has low toxicity to human normal lymphocytes, and can be used in the preparation of drugs that inhibit the proliferation of HIV virus.

Description

technical field [0001] The present invention relates to the field of biochemistry, and more specifically relates to a compound and its preparation method and application. Background technique [0002] AIDS, Acquired Immunodeficiency Syndrome, is an infectious disease caused by human immunodeficiency virus (HIV) infection. HIV is a virus that attacks the body's immune system. It takes the most important T4 lymphoid tissue in the human immune system as an attack target, destroys T4 lymphoid tissue in large quantities, and produces highly fatal internal failure. This virus spreads throughout the region for life, destroys the immune balance of people, and makes the human body a carrier of various diseases. [0003] HIV itself does not cause any disease, but when the immune system is destroyed by HIV, the human body loses the opportunity to replicate immune cells due to low resistance, and is infected with other diseases, resulting in various co-infections and death. [0004] ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C303/38C07C311/21A61K31/18A61P31/18
Inventor 汪志勇徐坤王斌李丽君鲍亚捷孙琦
Owner UNIV OF SCI & TECH OF CHINA