Berberine-oryzanol compound, and preparation method and application thereof
A compound and synthesis method technology, applied in the field of drug synthesis, can solve the problems of inconvenient administration, large dosage, unsatisfactory absorption, etc., and achieve the effects of improved fat solubility, easy industrialization, and simple synthesis method
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Embodiment 1
[0023] Embodiment 1 prepares berberine (1)
[0024] According to the synthetic route of formula (II),
[0025]
[0026] In the formula, n=1, X=CH, Y=C=O.
[0027] Dissolve oryzanol (3) in pyridine, slowly add berberine-8-acetyl chloride (2) at room temperature, stir at room temperature for 4 hours after the addition is completed, and pour the reaction mixture into stirring ice water to precipitate Crystallized, filtered, washed with water and dried to obtain crude product. Take the crude product and recrystallize it with ethanol to obtain the fine product of berberine (1).
Embodiment 2
[0028] Embodiment 2 prepares berberine (1)
[0029] According to the synthetic route of formula (II),
[0030]
[0031] In the formula, n=1, X=CH, Y=CH 2
[0032] Dissolve 8-chloroethyl berberine (2) in DMF, add oryzanol sodium salt, stir at 40°C for 10 hours, after the reaction is complete, pour the mixture into ice water under stirring, precipitate crystals, filter, wash with water, and dry , get crude products. Take the crude product and recrystallize it with ethanol to obtain the fine product of berberine (1).
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