Berberine and its derivatives and synthetic method
A derivative, the technology of barberry, which is applied in the field of compound drug synthesis, can solve the problems of poor absorption, suboptimal drug absorption, large drug dose, etc., and achieve the goal of overcoming poor absorption by the human body, improving blood indicators, and simple synthesis method Effect
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Embodiment 1
[0025] Prepare hydrogenated berberine according to the following formula (2)
[0026]
[0027] Wherein, n=1, X=CH, Y=CH 2 C=O
[0028] Dissolve oryzanol (4) in pyridine, slowly add berberine-8-acetyl chloride (3) at room temperature, and stir at room temperature for 4 hours after the addition is complete. After the reaction is complete, 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 hydrogenated berberine (2).
Embodiment 2
[0030] Prepare hydrogenated berberine according to the following formula (2)
[0031]
[0032] Wherein, n=1, X=CH, Y=CH 2
[0033] Dissolve 8-chloroethyl berberine (3) 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 refined product of hydrogenated berberine (2).
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