A kind of random copolymer based on polyphosphate, its preparation method and application
A technology of random copolymers and polyphosphate esters, which can be used in medical preparations, drug combinations, and pharmaceutical formulations of non-active ingredients, and can solve problems such as no reports on phosphate ester copolymers.
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Embodiment 1
[0050] Example 1: Random copolymer Poly(CL) with side groups having carbon-carbon double bonds 26 - co -OPEA 6 )Synthesis
[0051] Initiation of the monomer ε-caprolactone (ε-CL) and the phosphate monomer 2-acrylate ethyloxy-2-oxo-1,3,2-dioxaphospholane (OPEA) with benzyl alcohol Ring-opening copolymerization to prepare a random copolymer Poly(CL 26 - co -OPEA 6 ).
[0052] Dry the branched round-bottomed flask with a stirrer in an oven at 120°C for at least 24 hours, plug it with a glass stopper, connect it to an oil pump through a latex tube and pump it to room temperature, then introduce high-purity argon gas, and then evacuate it. After repeating three times, it was filled with argon.
[0053] Benzyl alcohol (0.10 g, 0.93 mmol), ε-caprolactone (ε-CL) (4.51 g, 39.43 mmol), OPEA (2.24 g, 10.08 mmol), toluene (10 mL) were sequentially injected from the branch tube with a dry syringe and stannous octoate [Sn(Oct) 2 ] (12 mg). After the reaction bottle was filled with...
Embodiment 2
[0054] Example 2: Random copolymer Poly[CL with carboxyl groups in side groups 26 - co -(OPEA -COOH ) 6 ]Synthesis
[0055] The Poly(CL of embodiment one preparation 26 - co -OPEA 6 ) and the thiol reagent mercaptopropionic acid under the irradiation of 365nm ultraviolet light to carry out the mercapto-alkene addition reaction to obtain the random copolymer Poly[CL 26 - co -(OPEA -COOH ) 6 ].
[0056] Add Poly(CL 26 - co -OPEA 6 ) (0.52g, 0.12mmol), add chloroform to dissolve, then add mercaptopropionic acid (0.12g, 1.08mmol) and photoinitiator benzoin dimethyl ether (DMPA) (1mg) in turn, and place it under a 365nm ultraviolet lamp to react 30 minutes. Shake the reaction dish gently every 5 minutes during the reaction to complete the reaction. After the reaction was completed, the reaction mixture was precipitated with 100 mL of ice anhydrous ether, and the ether was poured off to obtain a colorless viscous substance. Dry the crude product in a vacuum oven for ...
Embodiment 3
[0057] Example 3: Random copolymer Poly[CL with galactose groups in side groups 26 - co -(OPEA -Gal ) 6 ]Synthesis
[0058] Using galactosamine hydrochloride as the amino reagent, in 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC·HCl) and N-hydroxysuccinimide (NHS ) in the presence of Poly[CL 26 - co -(OPEA -COOH ) 6 ] carboxyl group to undergo amidation reaction to obtain a random copolymer Poly[CL with liver cell targeting and biodegradability 26 - co -(OPEA -Gal ) 6 ].
[0059] In a 25mL dry three-necked flask, add Poly[CL 26 - co -(OPEA-COOH) 6 ] (0.23g, 0.05mmol), 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC·HCl) (0.16g, 0.83mmol) and N-hydroxysuccinyl Imine (NHS) (0.08 g, 0.69 mmol), dissolved in 10 mL of dry dimethyl sulfoxide (DMSO), was activated for 12 h. Triethylamine (0.07g, 0.69mmol) and galactosamine hydrochloride (0.11g, 0.51mmol) were dissolved in 5mL of DMSO, and added dropwise to the reaction bottle. After the...
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