Composition of protein and double chain polyethylene glycol
A polyethylene glycol and protein technology, applied in the field of polyethylene glycol, can solve the problems of poor biological activity of conjugates, loss of beneficial properties, disconnection of linkers, etc., and achieve the effect of reducing immunogenicity and not being easy to hydrolyze and break
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Embodiment 1
[0017] Embodiment 1: the preparation of N, N-dipolyethylene glycol acetamido-methic acid succinimidyl ester 4000 (Bis-PEG4000)
[0018] Dissolve 10g of monomethoxypolyethylene glycol amine 4000 in 50ml of toluene, dissolve 500mg of TSAT (triethylamine trisuccinate) in 5ml of DMSO, add dropwise in 50ml of toluene, and react the resulting mixture for 16 hours under electromagnetic stirring , evaporate most of the solvent in vacuo. The resulting precipitate was redissolved in 100 ml of ethyl acetate at 60°C, and placed at 4°C for recrystallization. The filtered crystals were dried in a vacuum dryer to obtain 8.7 g of Bis-PEG white powder.
Embodiment 2
[0019] Embodiment 2: the preparation of N, N-dipolyethylene glycol acetamido-methic acid succinimidyl ester 8000 (Bis-PEG8000)
[0020] Dissolve 20g of monomethoxypolyethylene glycol amine 8000 in 50ml of toluene, dissolve 500mg of TSAT (triethylamine trisuccinate) in 5ml of DMSO, add dropwise in 50ml of toluene, and react the resulting mixture for 16 hours under electromagnetic stirring , evaporate most of the solvent in vacuo. The resulting precipitate was redissolved in 100 ml of ethyl acetate at 60°C, and placed at 4°C for recrystallization. The filtered crystals were dried in a vacuum desiccator to obtain 16.5 g of Bis-PEG white powder.
Embodiment 3
[0021] Embodiment 3: Preparation of N, N-dipolyethylene glycol acetamido-methic acid succinimidyl ester 20000 (Bis-PEG20000)
[0022] Dissolve 40g of monomethoxypolyethylene glycol amine 20000 in 80ml of toluene, dissolve 500mg of TSAT (triethylamine trisuccinate) in 5ml of DMSO, add dropwise in 50ml of toluene, and react the resulting mixture for 16 hours under electromagnetic stirring , evaporate most of the solvent in vacuo. The resulting precipitate was redissolved in 100 ml of ethyl acetate at 60°C, and placed at 4°C for recrystallization. The filtered crystals were dried in a vacuum dryer to obtain 32.1 g of Bis-PEG white powder.
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