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Gastrodin derivatives, their preparation methods, their applications and pharmaceutical preparations

A kind of pharmaceutical preparation, technology of gastrodin, applied in the field of gastrodin

Active Publication Date: 2018-11-27
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, currently there are few reports on the structural modification of gastrodin aglycon and the development of drugs with cardiovascular and cerebrovascular applications.

Method used

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  • Gastrodin derivatives, their preparation methods, their applications and pharmaceutical preparations
  • Gastrodin derivatives, their preparation methods, their applications and pharmaceutical preparations
  • Gastrodin derivatives, their preparation methods, their applications and pharmaceutical preparations

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preparation example Construction

[0044] The present invention also provides a preparation method of gastrodin derivatives, comprising:

[0045] Under the action of a catalyst, the compound having the structure of formula (XI) is reacted with the compound having the structure of formula (XII) in a solvent to obtain a gastrodin derivative having the structure of formula (II);

[0046]

[0047] R-OH (Ⅻ);

[0048]

[0049] Wherein, R is a substituted indene ring.

[0050] In the process of preparing gastrodin derivatives, the compound of formula (XI) is tetraacetylglucose trichloroacetimidate, which can be prepared according to the preparation method well known to those skilled in the art, and this application has no special limits. The molar ratio of the tetraacetylglucose trichloroacetimidate to the compound having the structure of formula (XII) is preferably 2 to 3:1, the reaction temperature is preferably 20 to 30°C, and the reaction time is Preferably it is 1-3h. The reaction process of gastrodin d...

Embodiment 1

[0065] The preparation of embodiment 1KPC-4000006

[0066]

[0067] In a 25ml two-necked flask, add compound 1 (150mg, 1.0mmol, 1.0eq), compound 2 (748mg, 1.52mmol, 1.5eq) and molecular sieves (3.0g, 4A), use the vacuum oil pump to remove the air inside the reaction device Replaced with nitrogen, added dichloromethane (5.0ml) to the flask successively, placed the flask in an ice bath, and stirred for 30 minutes; slowly added boron trifluoride diethyl ether (0.15mL, 1.21mmol, 1.2eq ); continue stirring for 30 minutes after the dropwise addition, then remove the ice bath, allow the reaction solution to naturally warm up to room temperature (20°C), and use TLC to detect the reaction process until the raw material disappears (2 hours); slowly pour the reaction solution into a A beaker filled with crushed ice (20g) was quenched, and until the ice cubes melted completely, the aqueous phase of the resulting mixed solution was extracted with ethyl acetate (20ml×3); the organic phas...

Embodiment 2

[0069] The preparation of embodiment 2KPC-4000007

[0070]

[0071] In a 25ml two-necked flask, add compound 4 (150mg, 1.0mmol, 1.0eq), compound 2 (748mg, 1.52mmol, 1.5eq) and molecular sieves (3.0g, 4A), use the vacuum oil pump to remove the air inside the reaction device Replaced with nitrogen, added dichloromethane (5.0ml) to the flask successively, placed the flask in an ice bath, and stirred for 30 minutes; slowly added boron trifluoride diethyl ether (0.15mL, 1.21mmol, 1.2eq ), continue to stir for 30 minutes after the dropwise addition; then remove the ice bath, allow the reaction solution to naturally warm up to room temperature (20 ° C), and use TLC to detect the reaction process until the raw materials disappear (2 hours); slowly pour the reaction solution into a A beaker filled with crushed ice (20g) was quenched, and until the ice cubes melted completely, the aqueous phase of the resulting mixed solution was extracted with ethyl acetate (3×20ml), the organic pha...

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Abstract

The invention provides a gastrodin derivative and a preparation method thereof. The gastrodin derivative contains substituted indene ring. The invention also provides a preparation method of the gastrodin derivative. A turbidimetry is used for determining a platelet aggregation rate so as to evaluate an inhibition rate of the gastrodin derivative for the platelet aggregation. An experiment result shows that the gastrodin derivative has an obvious anticoagulation effect and can be used as a potential lead compound in preparing drugs for treating thrombus, cardiovascular and cerebrovascular diseases, stroke and other diseases associated with blood coagulation.

Description

technical field [0001] The invention relates to the technical field of gastrodin, in particular to gastrodin derivatives, their preparation methods, their applications and pharmaceutical preparations. Background technique [0002] Cardiovascular and cerebrovascular diseases are a common disease that seriously threatens human beings, especially the health of middle-aged and elderly people. The number of people who die from cardiovascular and cerebrovascular diseases in the world is as high as 15 million every year, ranking first among various causes of death. At present, there are more than 270 million patients with cardiovascular and cerebrovascular diseases in my country, and nearly 3 million people die from cardiovascular and cerebrovascular diseases in China every year, accounting for 51% of the total annual death causes in my country. Cardiovascular and cerebrovascular diseases have become the number one killer with the highest cause of death for human beings, and they a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H15/203C07H1/00A61K31/704A61P7/02A61P9/00A61P9/10A23L33/105
CPCA23V2002/00C07H1/00C07H15/203A23V2200/326
Inventor 李剑峰周思雨王贤坝德伟杨兆祥张建文黄茜
Owner KPC PHARM INC
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