Polyethylene glycol-aliphatic saturated polyester block copolymer with aldehyde group-containing side chain and application thereof
A polyethylene glycol and polyester block technology, which can be used in medical preparations containing active ingredients, medical preparations without active ingredients, organic active ingredients, etc., can solve problems such as inability to pH, response, etc. , improve the stability, improve the effect of drug release performance
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Embodiment 1
[0024] (a) Preparation of polyethylene glycol-aliphatic saturated polyester block copolymers containing aldehyde groups in the side chain
[0025] Add 2g (0.001mol) of polyethylene glycol monomethyl ether with a molecular weight of 2000, 2g (0.02mol) of succinic anhydride, 2.28g (0.02mol) of allyl glycidyl ether and 43.8mg (0.2mmol) of zinc acetate into 10mL In DMF, after three freeze-thaw cycles, under the protection of nitrogen, the temperature was raised to 90°C for ring-opening polymerization for 9 hours, cooled to room temperature, and added to cold ethanol for precipitation to obtain a polyethylene glycol-aliphatic saturated polyester block copolymer;
[0026] Get 2g of the above polyethylene glycol-aliphatic saturated polyester block copolymer, 1.26g (0.00955mol) 3-mercapto-2-methylpentanal and 0.1g phenylbis(2,4,6-trimethyl Benzoyl)phosphine oxide was added to 10 mL of THF, irradiated with 365 nm ultraviolet light for 2 h, dialyzed, and freeze-dried to obtain a polyeth...
Embodiment 2
[0047] (a) Preparation of polyethylene glycol-aliphatic saturated polyester block copolymers containing aldehyde groups in the side chain
[0048] Add 2g (0.001mol) of polyethylene glycol monomethyl ether with a molecular weight of 2000, 3g (0.03mol) of succinic anhydride, 3.42g (0.03mol) of allyl glycidyl ether and 65.7mg (0.3mmol) of zinc acetate into 10mL In DMF, after three freeze-thaw cycles, under the protection of nitrogen, the temperature was raised to 90°C for ring-opening polymerization for 8.5 hours, cooled to room temperature, and added to cold methanol for precipitation to obtain polydiethanol-aliphatic saturated polyester copolymer;
[0049] Get 2g of the above polyethylene glycol-aliphatic saturated polyester copolymer, 2.8g (0.0214mol) 3-mercapto-2-methylpentanal and 0.2g phenyl bis(2,4,6-trimethylbenzyl Acyl)phosphine oxide was added to 10 mL of THF, irradiated with 365 nm ultraviolet light for 2 h, dialyzed, and freeze-dried to obtain a polyethylene glycol-al...
Embodiment 3
[0061] (a) Preparation of a side chain polyethylene glycol-aliphatic saturated polyester block copolymer containing aldehyde groups
[0062] Add 2g (0.001mol) of polyethylene glycol monomethyl ether with a molecular weight of 2000, 2.5g (0.025mol) of succinic anhydride, 2.85g (0.025mol) of allyl glycidyl ether and 54.75mg (0.25mmol) of zinc acetate In 10mL DMF, after three freeze-thaw cycles, under nitrogen protection, the temperature was raised to 90°C for ring-opening polymerization for 8 hours, cooled to room temperature, and added to cold methanol for precipitation to obtain polyethylene glycol-aliphatic saturated polyester block copolymer;
[0063] Get 2g of the above polyethylene glycol-aliphatic saturated polyester block copolymer, 1.8g (0.0136mol) 3-mercapto-2-methylpentanal and 0.2g phenylbis(2,4,6-trimethyl Benzoyl)phosphine oxide was added to 10 mL of THF, irradiated with 365 nm ultraviolet light for 2 h, dialyzed, and freeze-dried to obtain a polyethylene glycol-al...
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