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(R)-2-hydroxy-N-((2S,3S)-2-((R,E)-1-hydroxy pentadecane-4-alkene-1-yl)oxygen heterocycle-3-yl)lignoceric acid amino and preparation method thereof

A technology of tetracosanoic acid amine and hydroxypentadecane, which can be used in metabolic diseases, cardiovascular system diseases, organic chemistry, etc., can solve problems such as heavy economic burden, and achieve prevention of coronary heart disease, low drug prices, and prevention of arterial disease. Effects of atherosclerosis

Inactive Publication Date: 2016-08-17
QINGDAO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the existing drugs for the prevention and prevention of atherosclerosis are relatively expensive, and the economic burden for the common people in our country is relatively heavy.

Method used

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  • (R)-2-hydroxy-N-((2S,3S)-2-((R,E)-1-hydroxy pentadecane-4-alkene-1-yl)oxygen heterocycle-3-yl)lignoceric acid amino and preparation method thereof
  • (R)-2-hydroxy-N-((2S,3S)-2-((R,E)-1-hydroxy pentadecane-4-alkene-1-yl)oxygen heterocycle-3-yl)lignoceric acid amino and preparation method thereof
  • (R)-2-hydroxy-N-((2S,3S)-2-((R,E)-1-hydroxy pentadecane-4-alkene-1-yl)oxygen heterocycle-3-yl)lignoceric acid amino and preparation method thereof

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preparation example Construction

[0027] The present invention also provides a method for preparing a compound having a structure shown in formula (I), comprising the following steps:

[0028] 1) Put the bok choy in a round-bottomed beaker, add methanol, collect the alcohol extract, filter, and condense into a paste;

[0029] 2) adding water to the paste obtained in step 1) to obtain a suspension;

[0030] 3) Add petroleum ether and chloroform to the suspension described in step 2) respectively to obtain petroleum ether extract and chloroform extract respectively, and concentrate the petroleum ether extract and the chloroform extract to obtain thick paste, then add dextrin, dry under reduced pressure, that is.

[0031] In the present invention, methanol is added to beef vegetable, the alcohol extract is collected, filtered and concentrated into a paste. In the embodiment of the present invention, in order to repeatedly extract the alcohol extract in the beef and vegetable, the first methanol is added to the ...

Embodiment 1

[0043] Take 10kg beef vegetable, put it in a round bottom flask, add 40000mL of methanol, soak for 24h, heat and reflux for extraction for 5 hours, and collect the alcohol extract; add 40000mL of methanol to the remaining medicinal residues, heat and reflux for 5 hours, and take out the alcohol extract , combined two ethanol extracts, filtered, recovered methanol and continued to concentrate into a paste; added an appropriate amount of water to make the volume of the suspension 6000mL; then added petroleum ether and chloroform to extract the suspension, petroleum ether, The number of extractions with chloroform was 3 times, and the amount of petroleum ether and chloroform was 6000 mL each time. The extracted extract was concentrated into a thick paste, 0.069 g of dextrin was added, and dried under reduced pressure at 60 ° C to obtain the product.

Embodiment 2

[0045]Take 8kg beef vegetable, put it in a round bottom flask, add 35000mL of methanol, soak for 18h, heat and reflux for extraction for 4 hours, and collect the alcohol extract; add 35000mL of methanol to the remaining medicinal residues, heat and reflux for 5 hours, and take out the alcohol extract , combined two ethanol extracts, filtered, recovered methanol and continued to concentrate into a paste; added an appropriate amount of water to make the volume of the suspension 5500mL; then added petroleum ether and chloroform to extract the suspension, petroleum ether, The number of extractions with chloroform was 2 times, and the amount of petroleum ether and chloroform used each time was 5500mL. The extracted extract was concentrated into a thick paste, 0.06g of dextrin was added, and dried under reduced pressure at 50°C to obtain the product.

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Abstract

The invention discloses (R)-2-hydroxy-N-((2S,3S)-2-((R,E)-1-hydroxy pentadecane-4-alkene-1-yl)oxygen heterocycle-3-yl)lignoceric acid amino which is of a structure of formula (I) as shown in the specification. By adopting the structure, blood lipid can be regulated, atherosclerosis can be prevented, and coronary heart diseases can be prevented; moreover, the compound is simple in preparation method, low in medicine price and good in selective inhibition function on ACAT.

Description

technical field [0001] The invention relates to the field of preventing atherosclerosis, in particular to a (R)-2-hydroxyl-N-((2S,3S)-2-((R,E)-1-hydroxypentadecane-4-ene -1-yl)oxetan-3-yl)tetracosanoic acid amine and its preparation method. Background technique [0002] Cardiovascular disease ranks among the three major diseases that currently threaten human health, namely, cardiovascular disease, tumors and infectious diseases, and atherosclerosis is one of the most important pathological bases of cardiovascular disease. The main causes of death from cardiovascular and cerebrovascular diseases such as infarction, cerebral infarction and coronary heart disease are related to the occurrence and development of many diseases. Prevention and treatment of atherosclerosis is the fundamental measure to prevent and treat cardiovascular diseases. The development of anti-arteriosclerosis vaccine will help to inhibit the occurrence and development of arteriosclerosis, help reduce the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D305/08A61P3/06A61P9/10
CPCC07D305/08
Inventor 王春波姜启晓王龙源陈雪红
Owner QINGDAO UNIV
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