Acyclovir-chitosan-stearic acid grafting, synthetic method and application thereof
A technology of stearic acid and chitosan, which is applied in the application field of preparing anti-hepatitis B virus drugs, can solve the problems of limited drug loading capacity and difficult loading, and achieve the effects of increasing drug concentration, increasing intake, and reducing toxic and side effects
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Embodiment 1
[0020] Embodiment 1: the synthesis of acyclovir-chitosan-stearic acid graft
[0021] (1) Synthesis of acyclovir-succinic acid intermediate: 562.5mg (2.5mmol) acyclovir, 500.0mg (5.0mmol) succinic anhydride and 0.355mL triethylamine were dissolved in 37.5mL dry N , N-dimethylformamide, 60 ℃ water bath reaction 21h. After the reaction solution was cooled, most of the volatile components were evaporated under reduced pressure, 25 mL of ice water was added, and 2N hydrochloric acid was added to adjust the pH to 2. The white precipitate was collected by filtration, washed thoroughly with ice water, and dried at 40°C. Put the white precipitate into a round-bottomed flask, add a small amount of methanol, stir in a water bath at 70°C, reflux with a condenser, slowly add methanol dropwise until the solids are completely dissolved, let stand overnight at room temperature, filter with suction to obtain white crystals, and dry at 40°C to obtain Acyclovir-succinic acid intermediate.
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Embodiment 2
[0026] Embodiment 2: the synthesis of acyclovir-chitosan-stearic acid graft
[0027] (1) Synthesis of acyclovir-succinic acid intermediate: 562.5mg (2.5mmol) acyclovir, 500.0mg (5.0mmol) succinic anhydride and 0.355mL triethylamine were dissolved in 37.5mL dry N , N-dimethylformamide, 60 ℃ water bath reaction 21h. After the reaction solution was cooled, most of the volatile components were evaporated under reduced pressure, 25 mL of ice water was added, and 2N hydrochloric acid was added to adjust the pH to 2. The white precipitate was collected by filtration, washed thoroughly with ice water, and dried at 40°C. Put the white precipitate into a round-bottomed flask, add a small amount of methanol, stir in a water bath at 70°C, reflux with a condenser, slowly add methanol dropwise until the solids are completely dissolved, leave it at room temperature overnight, filter with suction to obtain white crystals, and dry at 40°C to obtain Acyclovir-succinic acid intermediate.
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Embodiment 3
[0036] Embodiment 3: the synthesis of acyclovir-chitosan-stearic acid graft
[0037] (1) Synthesis of acyclovir-succinic acid intermediate: 562.5mg (2.5mmol) acyclovir, 500.0mg (5.0mmol) succinic anhydride and 0.355mL triethylamine were dissolved in 37.5mL dry N , N-dimethylformamide, 60 ℃ water bath reaction 21h. After the reaction solution was cooled, most of the volatile components were evaporated under reduced pressure, 25 mL of ice water was added, and 2N hydrochloric acid was added to adjust the pH to 2. The white precipitate was collected by filtration, washed thoroughly with ice water, and dried at 40°C. Put the white precipitate into a round-bottomed flask, add a small amount of methanol, stir in a water bath at 70°C, reflux with a condenser, slowly add methanol dropwise until the solids are completely dissolved, let stand overnight at room temperature, filter with suction to obtain white crystals, and dry at 40°C to obtain Acyclovir-succinic acid intermediate.
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