Intestine targeted formulation of PEGylated rotavirus and its synthesizing method
A technology of PEGylation and rotavirus, applied in the direction of antiviral agents, antiviral immunoglobulins, antibodies, etc., can solve the problems of low bioavailability, immune response, short half-life, etc., to reduce immunogenicity, Effect of reducing toxicity and increasing stability
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[0035] (1) Synthesis of Polyethylene Glycol PEG Activated Intermediate
[0036] Step 1: Synthesis of omega-methoxypolyethylene glycol
[0037]
[0038] Under the condition of 0--100°C, add methyl bromide into the organic solvent of polyethylene glycol (molar ratio 1:1), stir, react for 2-10 hours, remove the organic solvent in vacuum, and separate the residue by column chromatography , TLC (iodine color) detection, the product was obtained.
[0039] The second step: the synthesis of omega-methoxy polyethylene glycol monoester
[0040]
[0041] name
molecular weight
The molar ratio of
Feeding amount
moles
MePEG2000
2000
1
100g
0.05
100
3
15g
0.15
101
2
14ml
0.1
DMAP
122
1.1
6.8g
0.055
500ml
[0042] Polyethylene glycol MePEG 2000 , succinic anhydride, DMAP, dichl...
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