A kind of preparation method and application of triptolide-carboxylated chitosan coupling drug
A technology for carboxylating chitosan couple and triptolide, which is applied in the field of medicine, can solve the problems of large toxic and side effects, poor water solubility, short biological half-life and the like of triptolide, and achieves remarkable economic and social benefits, simple method, The effect of long biological half-life
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Embodiment 1
[0017] Embodiment 1: the preparation method of a kind of triptolide-carboxylated chitosan coupling drug of the present invention comprises the following steps: (1), the synthesis of intermediate carboxylated triptolide (TP-L3): 1800mg (5mmol) of triptolide was dissolved in 10ml of pyridine, then 1720mg (20mmol) of malonic anhydride and 122mg (1mmol) of 4-dimethylaminopyridine (DMAP) were added, under the protection of nitrogen, the reaction was carried out at room temperature for 24h, and 100mL of dichloromethane, then washed with saturated copper sulfate solution and water for 1-3 times, take the organic phase, dry the organic phase with anhydrous sodium sulfate, and then use a volume ratio of CH 2 Cl 2 :CH 3 The mixture of OH=20-15:1 was used as the mobile phase for silica gel chromatography column purification, and then recrystallized from dichloromethane-acetone-ether to obtain the hydroxyl-functional intermediate carboxylated triptolide (TP-L3) ;
[0018] (2), triptoli...
Embodiment 2
[0019] Embodiment 2: the preparation method of a kind of triptolide-carboxylated chitosan coupling drug of the present invention comprises the following steps: (1), the synthesis of intermediate carboxylated triptolide (TP-L4): 360mg (1mmol) of triptolide was dissolved in 5ml of pyridine, then 400mg (4mmol) of succinic anhydride and 24mg (0.2mmol) of 4-dimethylaminopyridine (DMAP) were added, under the protection of nitrogen, the reaction was carried out at room temperature for 24h, and 60mL of dichloromethane, and then washed with saturated copper sulfate solution and water for 1-3 times, take the organic phase, dry the organic phase with anhydrous sodium sulfate, and then use a volume ratio of CH 2 Cl 2 :CH 3 The mixture of OH=20-15:1 was used as the mobile phase for silica gel chromatography column purification, and then recrystallized from dichloromethane-acetone-ether to obtain the hydroxyl-functional intermediate carboxylated triptolide (TP-L4) ;
[0020] (2), triptol...
Embodiment 3
[0021] Embodiment 3: the preparation method of a kind of triptolide-carboxylated chitosan coupling drug of the present invention comprises the following steps: (1), the synthesis of intermediate carboxylated triptolide (TP-L5): Dissolve 900mg (2.5mmol) of triptolide in 10ml of pyridine, then add 912mg (8mmol) of glutaric anhydride and 62mg (0.5mmol) of 4-dimethylaminopyridine (DMAP), and react for 24h under nitrogen protection and stirring at room temperature , add 100mL of dichloromethane, and wash with saturated copper sulfate solution and water for 1-3 times respectively, take the organic phase, dry the organic phase with anhydrous sodium sulfate, and then use a volume ratio of CH 2 Cl 2 :CH 3 The mixture of OH=20-15:1 was used as the mobile phase for silica gel chromatography column purification, and then recrystallized from dichloromethane-acetone-ether to obtain the hydroxyl-functional intermediate carboxylated triptolide (TP-L5) ;
[0022](2), triptolide-carboxylated...
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