A kind of phenol theophyllic acid and its preparation method and application

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: 2018-06-12
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 with placebo, memantine did not improve mild cognitive impairment in patients impairment and cognitive function, and it increases the risk of gastrointestinal damage

Method used

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  • A kind of phenol theophyllic acid and its preparation method and application
  • A kind of phenol theophyllic acid and its preparation method and application
  • A kind of phenol theophyllic acid and its preparation method and application

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 present invention relates to a kind of phenol theophyllic acid and its preparation method and application; 5 millimoles of dihydromyricetin is added to 20 milliliters of methanol and dissolved for 30 minutes, the dissolved solution is placed in an ice bath, and 5.5 millimoles of piperidine is added to the Titrate into the dihydromyricetin methanol solution in the presence of argon at ‑10°C, let it stand for 20 minutes to make it react completely, then concentrate the reaction solution under vacuum to reduce the air pressure by 20%, filter it, and wash it three times with methanol. Phenolic acid is available; it can be used as a therapeutic drug for Alzheimer's dementia and other neurological / nervous system progressive degenerative diseases; phenolic acid is a potential drug for effective prevention and treatment of Alzheimer's dementia Compound; can effectively improve anxiety, cognitive disorders, sleep disorders, cognition caused or occurred due to various reasons, and other forms of functional decline symptoms of learning / memory ability; its structural formula is as follows:

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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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/32C07D295/027C07D295/023A61P25/28A61P25/22A61P25/20
CPCC07D295/023C07D295/027C07D311/32
Inventor 梁京
Owner 梁京
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