Phenol tea acid and preparation method and application thereof

A technology of phenol theophyllic acid and dihydromyricetin, applied in organic chemistry, nervous system diseases, drug combination, etc., can solve the problems of increasing gastrointestinal tract damage and failing to improve patients' mild cognitive impairment and cognitive function

Active Publication Date: 2016-06-29
梁京
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In a systematic review of the safety of memantine, memantine was tried to treat mild cognitive impairment in Alzheimer's dementia, but the results showed that compared

Method used

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  • Phenol tea acid and preparation method and application thereof
  • Phenol tea acid and preparation method and application thereof
  • Phenol tea acid and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0093] Synthesized five millimoles (5 mmol, 1.6 g) of dihydromyricetin were added to 20 ml of methanol and dissolved for 30 minutes, and the dissolved solution was placed in an ice bath. Use 5.5 mmol of piperidine (0.47 g / L), titrate into dihydromyricetin methanol solution in the presence of argon at -10°C, and let it stand for 20 minutes to make the reaction complete. Then, the reaction solution was concentrated under low pressure (vacuumizing to reduce the air pressure by about 20%), filtered, and washed three times with methanol to obtain phenotheophyllic acid (~2g).

Embodiment 2

[0095] 500 grams of dihydromyricetin was added to 6.25 liters of methanol to dissolve for 30 minutes, and the dissolved solution was placed in an ice tank. Use 103.8 g / L of piperidine to titrate into dihydromyricetin methanol solution in the presence of argon at -10°C, and let it stand for 20 minutes to make the reaction complete. Then, the reaction solution was concentrated under low pressure (vacuumizing to reduce the air pressure by about 20%), filtered, and washed three times with methanol to obtain phenol-theophyllic acid (about 625 grams).

Embodiment 3

[0097] 5000 grams of dihydromyricetin was added to 62.5 liters of methanol to dissolve for 30 minutes, and the dissolved solution was placed in an ice tank. Use 1038 g / L of piperidine to titrate into dihydromyricetin methanol solution in the presence of argon at -10°C, and let it stand for 20 minutes to make the reaction complete. Then, the reaction solution was concentrated under low pressure (vacuumizing to reduce the air pressure by about 20%), filtered, and washed three times with methanol to obtain phenol-theophyllic acid (about 6250 grams).

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Abstract

The invention relates to phenol tea acid and a preparation method and application thereof; the preparation method comprises: adding 5 mmol of dihydromyricetin into 20 ml of methyl alcohol, dissolving for 30 min, placing the dissolved solution in an ice cell, titrating 5.5 mmol of piperidine into the dihydromyricetin methyl alcohol solution in the presence of argon at -10 DEG C, placing for 20 min so that reaction is thorough, evacuating, concentrating reaction liquid under the air pressure decreased by 20%, filtering, and washing three times with methyl alcohol to obtain the phenol tea acid; the phenol tea acid is useful as a therapeutic drug for treating Alzheimer disease and other nervous/nervous system progressive degenerative changes; the phenol tea acid is a compound potentially effective in preventing and treating Alzheimer disease; the phenol tea acid is effective in improving anxiety disorder, cognitive disorder, sleep disorder, and cognitive, learning and memory ability functional degradative symptoms in other forms due to various reasons; the phenol tea acid has a following structural formula.

Description

technical field [0001] The invention relates to a phenol theophyllic acid and a preparation method thereof, which can be used as a therapeutic drug for Alzheimer's disease (Alzheimer's disease) dementia and other progressive degenerative diseases of the nervous system / nervous system. Background technique [0002] There are currently 36 million people worldwide living with Alzheimer's disease. One in nine people over the age of 65 in the world has dementia symptoms. In 2013, the socioeconomic burden related to Alzheimer's dementia exceeded 2.2 trillion US dollars, and Alzheimer's dementia is the most Common dementias, accounting for 50% to 75% of all dementias, increase with age. According to the 2013 report of the World Health Organization, more than 25%-50% of the 85-year-olds in the world suffer from Alzheimer's dementia. For people over 60 years old, dementia (mainly including Alzheimer's) is twice as common in low / middle-income areas as it is in high-income areas. The...

Claims

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Application Information

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IPC IPC(8): C07D311/32C07D295/027C07D295/023A61P25/28A61P25/22A61P25/20
CPCC07D295/023C07D295/027C07D311/32
Inventor 梁京
Owner 梁京
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