A kind of acetylated sugar ester-polyethylene glycol-phosphatidylethanolamine conjugate and its preparation method and application
A technology of phosphatidylethanolamine conjugates and distearoylphosphatidylethanolamine, applied in the field of medicine, can solve the problems that hinder the application and effect of solid tumor treatment, and the mechanism has not been fully understood
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Embodiment 1
[0068] Example 1 Synthesis of targeting molecule diisoamylphosphoethanolamine-polyethylene glycol-1000-p-p-carboxyphenyl-α-D-acetylmannosamine (DSPE-PEG-1000-Ac4MAN)
[0069]
[0070] Azide-polyethylene glycol-glutaric acid amide 1000 (1.3 g) was dissolved in tetrahydrofuran (20 mL), then Pd / c (0.066 g) and acetic acid (1 mL) were added, hydrogen gas was introduced at room temperature, and the reaction was carried out overnight. After the crude product was filtered, it was rotary evaporated to dryness, then dissolved in dichloromethane (20 mL), triethylamine (TEA, 0.65 mL) and Ac 4 MAN (1.5g) was reacted overnight at room temperature. Go through the column to get PEG1000-Ac 4MAN (1.18 g), 62% yield. Dissolve PEG 1000-Ac4MAN (1.18g) in dichloromethane, add NHS (0.2g) and EDCI (0.45g) in sequence, react overnight at room temperature, and pass through the column to obtain succinimide polyethylene glycol acetyl mannoside (1.0 g), 78% yield. Dissolve succinimide polyethylene...
Embodiment 2
[0072] Example 2 Targeting molecule Diisoamylphosphoethanolamine-polyethylene glycol-600-p-p-carboxyphenyl-α-D-acetylmannosamine (DSPE-PEG-600-Ac 4 MAN) synthesis
[0073]
[0074] Azide-polyethylene glycol-glutaric acid amide 600 (1.3 g) was dissolved in tetrahydrofuran (20 mL), then Pd / c (0.078 g) and acetic acid (1 mL) were added, hydrogen gas was introduced at room temperature, and the reaction was carried out overnight. After the crude product was filtered, it was rotary evaporated to dryness, then dissolved in dichloromethane (20 mL), added triethylamine (TEA, 0.79 mL) and Ac4MAN (1.7 g), and reacted overnight at room temperature. After passing through the column, PEG600-Ac4MAN (1.08 g) was obtained with a yield of 62%. Dissolve PEG 600-Ac4MAN (0.95g) in dichloromethane (20mL), add NHS (0.3g) and EDCI (0.51g) in sequence, react overnight at room temperature, and pass through the column to obtain succinimide polyethylene glycol Acetyl mannoside (0.82 g), 80% yield. ...
Embodiment 3
[0076] Example 3 Targeting molecule Diisoamylphosphoethanolamine-polyethylene glycol-2000-p-p-carboxyphenyl-α-D-acetylmannosamine (DSPE-PEG-2000-Ac 4 MAN) synthesis
[0077]
[0078] Azide-polyethylene glycol-glutaric acid amide 2000 (1.3 g) was dissolved in tetrahydrofuran (20 mL), then Pd / c (0.052 g) and acetic acid (1 mL) were added, hydrogen gas was introduced at room temperature, and the reaction was carried out overnight. After the crude product was filtered, it was rotary evaporated to dryness, then dissolved in dichloromethane (20 mL), added triethylamine (TEA, 0.54 mL) and Ac4MAN (1.34 g), and reacted overnight at room temperature. Through the column, PEG2000-Ac4MAN (1.15 g) was obtained with a yield of 63%. Dissolve PEG 2000-Ac4MAN (0.95g) in dichloromethane (20mL), add NHS (0.09g) and EDCI (0.19g) in turn, react overnight at room temperature, and pass through the column to obtain succinimide polyethylene glycol Acetylmannoside (0.87g), 82% yield. Add TEA (0.15...
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