Puerarin derivative and synthetic method and application thereof
A technology of puerarin derivatives and synthesis methods, which can be applied to drug combinations, medical preparations containing active ingredients, and pharmaceutical formulas, etc., which can solve the problem of low selectivity of pharmacological targets, improve learning and memory disorders, and balance internal and external Osmotic pressure, effect of improving fat solubility
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specific Embodiment approach 1
[0039] Specific embodiment one: Puerarin derivatives in this embodiment 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: In this embodiment, puerarin derivatives are represented by the 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 eluent with a volume ratio of dichloromethane to methanol of 40:1-15:1 is 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 hydrogen nuclear magnetic resonance spectrum of puerarin derivatives of structural formula (Ⅱ...
specific Embodiment approach 3
[0050] Specific embodiment three: In this embodiment, puerarin derivatives are represented by the following structural formula (Ⅲ):
[0051]
[0052] (Ⅲ), its synthetic method is carried 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 an oily state, grind with anhydrous acetone, Pour off the solvent anhydrous acetone, spin dry, dissolve in anhydrous methanol, and separate by silica gel column chromatography with an eluent with a volume ratio of dichloromethane to methanol of 15:1 to 10:1 to obtain the puerarin derivative of structural formula (Ⅲ) .
[0054] The puerarin derivatives described in this embodiment are used in the treatment of vascular dementia.
[0055] The H NMR spectra of puerarin derivatives of structural formula (Ⅲ) are shown i...
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