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Puerarin derivatives and their synthetic methods and applications

A technology of puerarin derivatives and synthesis methods, which can be used in drug combinations, medical preparations containing active ingredients, and pharmaceutical formulations, etc., can solve the problem of low selectivity of pharmacological targets, improve learning and memory disorders, balance internal and external The effect of osmotic pressure and improving fat solubility

Active Publication Date: 2016-02-03
HARBIN UNIV OF COMMERCE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The technical problem to be solved by the present invention is that although the prior art improves the water-solubility and fat-solubility of puerarin through modification, the selectivity of its pharmacological target is not high; however, puerarin derivatives and their synthesis methods and applications are provided

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  • Puerarin derivatives and their synthetic methods and applications
  • Puerarin derivatives and their synthetic methods and applications
  • Puerarin derivatives and their synthetic methods and applications

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Experimental program
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specific Embodiment approach 1

[0039] Specific embodiment one: in this embodiment, puerarin derivatives are represented by the following general formula (I):

[0040]

[0041] (I), where R 1 is hydrogen, cyano, cyanide, ethyl acetate or acetamide, R 2 is hydrogen, cyano, cyanide, ethyl acetate or acetamide, R 1 , R 2 Not simultaneously hydrogen.

[0042] The puerarin derivatives described in this embodiment are mainly produced by chemical synthesis methods such as addition reaction.

[0043] The puerarin derivatives described in this embodiment are used in the treatment of vascular dementia.

specific Embodiment approach 2

[0044] Specific embodiment two: the present embodiment puerarin derivative is represented by following structural formula (II):

[0045]

[0046] (II), its synthetic method is carried out according to the following steps:

[0047] Dissolve 36mmol puerarin in 200mL of absolute ethanol, add 216.3mmol K 2 CO 3 , stirred for 80min, added 216mmol chloroacetonitrile, stirred at room temperature for 10h, filtered (removed solid insolubles), rotary steamed into oil, ground with anhydrous ether, poured off anhydrous ether, spin-dried, dissolved with anhydrous methanol, and then used The eluate with a volume ratio of dichloromethane to methanol of 40:1-15:1 was subjected to silica gel column chromatography to obtain a puerarin derivative of structural formula (II).

[0048] The puerarin derivatives described in this embodiment are used in the treatment of vascular dementia.

[0049] The proton nuclear magnetic resonance spectra of the puerarin derivatives of structural formula (Ⅱ)...

specific Embodiment approach 3

[0050] Specific embodiment three: the puerarin derivative of this embodiment is represented by the following structural formula (Ⅲ):

[0051]

[0052] (Ⅲ), its synthetic method is to carry out according to the following steps:

[0053] Dissolve 36mmol of puerarin in 200mL of anhydrous DMF, add 216.3mmol of NaOH at room temperature, stir for 60min, add 216mmol of chloroacetonitrile, stir for 10h at room temperature, filter (remove solid insolubles), rotary steam to oil, grind with anhydrous acetone, pour The solvent was removed from anhydrous acetone, spin-dried, dissolved in anhydrous methanol, and separated by silica gel column chromatography with an eluent with a volume ratio of dichloromethane to methanol of 15:1 to 10:1 to obtain a puerarin derivative of structural formula (Ⅲ).

[0054] The puerarin derivatives described in this embodiment are used in the treatment of vascular dementia.

[0055] The proton nuclear magnetic resonance spectra of structural formula (Ⅲ) pu...

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Abstract

A puerarin derivative and a synthetic method and an application thereof belong to the field of cerebrovascular diseases. Selectivity of a vascular dementia therapeutic target is improved by decorating puerarin. The puerarin derivative is indicated through a formula (1) which is as follows. By means of a chemical synthetic method, products are applied to treatment of vascular dementia. Fat solubility and water solubility of the puerarin are improved, receptor selectivity of the puerarin is improved, osmotic pressures inside and outside brain cells are balanced, cellular swelling caused by inflammatory injury is improved, a pharmacologic action of the puerarin itself of improving microcirculation and cholinergic nerve system functions is highlighted, and learning and memory disorders caused by damage caused by ischemia reperfusion are avoided.

Description

technical field [0001] The present invention relates to a derivative and its synthesis method and application. Background technique [0002] Cerebrovascular disease is the most common disease in neurology, and it is also a common factor of adult disability. Coupled with the problem of population aging, the incidence of dementia is gradually increasing, which increases the burden on family and society. The main reason is the injury caused by ischemia-reperfusion. The morbidity of vascular dementia (VD) has increased most significantly, and vascular dementia has become the second largest dementia disease after Alzheimer's disease. According to foreign reports, VD is the only preventable dementia so far, and it will be reversible if treated early. Therefore, it has become an important subject of medical basic research and clinical research to explore the related factors and pathogenesis of VD in order to seek effective measures for early diagnosis, early prevention and early t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D407/04A61K31/352A61P25/28A61P9/10
Inventor 江培季宇彬
Owner HARBIN UNIV OF COMMERCE
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