Block copolymers and self-assembling nanoparticles formed therefrom
A technology of block copolymers and diblock copolymers, which is applied in the direction of drug combinations, medical preparations containing active ingredients, etc. Effectively penetrate issues such as
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Embodiment 1
[0078] Example 1 Acid and Urea Functionalized PEG-P (MTC-MAC)
[0079] 100 mg (0.5 mmol) of 5-methyl-5-allyloxycarbonyl-1,3-dioxan-2-one (MTC-MAC) was added to a solution containing In a reaction vial of 1-(3,5-bis(trifluoromethyl)-phenyl)-3-cyclohexyl-2-thiourea (TU) catalyst (9.25 mg, 0.025 mmol). To the mixture was added polyethylene glycol (PEG) (250 mg, 0.025 mmol, Mn 10,000 g / mol, PDI 1.04), followed by 1,8-diazabicyclo-[5,4,0]-undeca- 7-ene (DBU) (3.8 μL, 0.025 mmol), and stirred at room temperature for about 45 minutes.
[0080] At the end of the reaction, excess benzoic acid (5 mg, 0.04 mmol) was added to quench the catalyst. The crude polymer was then precipitated twice in cold ether and the supernatant was decanted to give a loose white powdery solid in 89% yield.
[0081] acid functionalization
[0082] Dissolve 200 mg (0.22 mmol olefin) of PEG-P (MTC-MAC) polymer in anhydrous N,N-dimethylformamide (DMF) (1 mL), then add 3-mercaptopropionic acid (57 μL, 0.66 mm...
Embodiment 2
[0087] Example 2 - Acid-functionalized PEG-P (MTC-MPC)
[0088] 99 mg (0.5 mmol) of 5-methyl-5-propargyloxycarbonyl-1,3-dioxan-2-one (MTC-MPC) was added to a solution containing TU catalyst (9.25 mg, 0.025 mmol) in a reaction vial. PEG (500 mg, 0.05 mmol, Mn 10,000 g / mol, PDI 1.04) was added to the mixture, followed by DBU (3.8 μL, 0.025 mmol), and stirred at room temperature for about 45 minutes.
[0089] At the end of the reaction, excess benzoic acid (5 mg, 0.04 mmol) was added to quench the catalyst. The crude polymer was then precipitated twice in cold ether and the supernatant was decanted to give a white powdery solid in 89% yield.
[0090] acid functionalization
[0091] Dissolve 198 mg (0.12 mmol alkyne) PEG-P(MTC-MPC) in anhydrous DMF, then add 3-mercaptopropionic acid (114 μL, 1.3 mmol) and 2,2-dimethoxy-2-phenyl Acetophenone (1.7 mg, 0.007 mmol) and mix.
[0092] The mixture was irradiated at 254 nm for two hours, precipitated twice in cold ether, and the supe...
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