Invisible polypeptide with good non-specific protein absorption resistance performance and preparation method thereof
A non-specific, protein-based technology, applied in the field of stealth polypeptides and their preparation, to achieve stealth performance and good anti-protein adsorption performance
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[0045] 1. Condensation
[0046] δ-(α-Benzyl-N ε Synthesis of -benzyloxycarbonyl-L-lysyl)-α-tert-butyl-N-tert-butoxycarbonyl-L-aspartic acid (4)
[0047] Dissolve H-Lys(Z)-OBzl·HCl (1, 6.10g, 15.0mmol) in 30mL of anhydrous DMF, add 2.5mL of TEA (18.10mmol), react with stirring for 20min, filter; then BOC-ASP -O t Bu (3, 4.34g, 15.0mmol), EDC·HCl (5.75g, 30.0mmol), HOBt (4.04g, 30mmol) were added to the filtrate, and after nitrogen protection for 30min, the reaction was sealed at room temperature for 48h; Most of the DMF was distilled off to obtain a yellow oil; the yellow oil was dissolved in ethyl acetate, washed successively with 10wt.% citric acid solution, saturated sodium bicarbonate solution, and saturated brine, and the organic phase was washed with anhydrous Dry over sodium sulfate, remove the solvent by rotary evaporation, and separate by silica gel column chromatography (mobile phase: dichloromethane / ethyl acetate=3:1, volume ratio) to obtain white solid (4) (7.80 ...
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