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Icariin derivative, and preparation method and application thereof

A technology of icariin and derivatives is applied in the preparation of sugar derivatives, sugar derivatives, sugar derivatives, etc., to achieve the effect of excellent medicinal effect

Inactive Publication Date: 2013-08-28
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] If new cholinesterase inhibitors can be found by improving the structure of icariin, it will bring good news to the treatment of Alzheimer's disease

Method used

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  • Icariin derivative, and preparation method and application thereof
  • Icariin derivative, and preparation method and application thereof
  • Icariin derivative, and preparation method and application thereof

Examples

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Embodiment 1

[0030] Example 1 Preparation of icariin derivatives of the present invention

[0031] Take 0.5g (0.74mmol, 1equiv) ICA in a 50mL flask, add it in 10mL methanol and stir to form a suspension for later use, take another 50mL flask and add 37% formaldehyde solution (10equiv), 2mL methanol to dilute, add dropwise with stirring ( 0.74mmol, 1equiv) secondary ammonia (structural formula is as follows), stirred at room temperature for 10min, slowly added the methanol suspension of ICA into the flask, heated to reflux for 12h, thin-layer monitoring, after the reaction was completed, concentrated in vacuo, the crude product was dissolved. It was washed with ethyl acetate and saturated brine, then washed with water, dried over anhydrous MgSO4, concentrated in vacuo, and subjected to column chromatography to obtain the nitrogen-containing derivative of icariin corresponding to secondary ammonia.

[0032] The structural formula of above-mentioned secondary ammonia is where R 1 , R 2 is...

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Abstract

The invention provides icariin derivatives disclosed in the specification, wherein R1 and R2 are respectively and independently selected from H and C1-C5 alkyl groups, or R1 and R2 with N connected with R1 and R2 jointly form a substituted or non-substituted 3-6-element ring or a 3-6-element ring containing more than two heteroatoms; and the substituent group is selected from C1-C5 alkyl groups. The icariin derivatives provided by the invention have in-vitro acetylcholine ester inhibiting activity, and have better drug effects than icariin, thereby providing a new option for clinical medicines for treating senile dementia.

Description

technical field [0001] The present invention relates to icariin derivatives and their preparation methods and uses. Background technique [0002] Alzheimer's disease (AD), the most common form of Alzheimer's disease, is a progressive neurodegenerative disease and one of the most common causes of mental deterioration in middle-aged and elderly people, with more than 250,000 people suffering from Alzheimer's disease disease. In the past few decades, a lot of research work has been devoted to exploring the pathogenesis of Alzheimer's disease and seeking drugs to treat Alzheimer's disease, and various hypotheses have been put forward one after another. Among them, the latest and most mainstream hypothesis is the theory of β-amyloid deposition. (Aβ). However, there is no new drug researched according to this theory on the market, and three new phase III clinical drugs targeting Aβ have been declared to have failed, which is a blow to the Aβ theory. At present, there are still ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/07C07H1/00A61K31/706A61K31/7056A61K31/7048A61P25/28
Inventor 尹述凡李霞陈超董林李颖
Owner SICHUAN UNIV
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