Pharmaceutical composition containing triacetyl andrographolidume and medical use of the same
A technology of andrographolide and triacetyl, used in immunosuppressive and anti-tumor drugs, in the field of preparation of anti-inflammatory
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[0006] 1. Preparation of triacetylandrographolide
[0007]
[0008] Add 5g (14.3mmol) of andrographolide (1), 20mL of acetic anhydride, and 2g of newly molten zinc chloride into a 100mL single-necked flask in sequence, attach a reflux condenser, and heat in an oil bath at 80°C. After the reaction solution was clarified, the reaction was stopped, and the reaction solution was poured into a beaker filled with 80 mL of ice water, stirred vigorously, filtered with suction, and the filter cake was washed with water to pH7. The filter cake was crystallized with ethanol to obtain 4.7 g of white needle crystals with a yield of 67.8%. m.p.128°C. IR (cm -1 ): 2976, 2955, 2925, 2868, 1753, 1736, 1680, 1450, 1375, 1251, 1026, 908. MS (ESI) m / z: 476.3M + , 477.3(M+1) + , 499.3 (M+Na) + . 1 H-NMR (CDCl 3 , δ): 7.01 (1H, t, J=5.2, 12-H), 5.91 (1H, d, J=6.0, 14-H), 4.90, 4.53, (each 1H, s, 17-H), 4.60 (1H, dd, J=6.1, 11.2, 15-H), 4.55 (1H, dd, J=5.0, 11.2, 15-H), 4.38, 4.14 (each ...
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