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目的合成具有酯水两性的脑靶向脂质体配体葡萄糖-胆固醇偶联物。方法将胆固醇3位羟基与对甲苯磺酰氯成酯后,与乙二醇取代,并氧化制得2-(5-胆甾烯-3-β-氧基)-1-乙酸,再与1,2,3,4-四-O-三甲硅基-β-D-吡喃葡萄糖在缩合剂DCC的作用下成酯,由三氟乙酸四氢呋喃溶液脱保护后得到目标配体。结果合成了1个葡萄糖胆甾偶联物。结论目标化合物以及重要中间体均经IR、1HNMR、MS等确证。
OBJECTIVE: To synthesize a brain-targeting liposome ligand glucose-cholesterol conjugate with ester-amphoteric properties. Methods Cholesterol 3-hydroxy ester with p-toluenesulfonyl chloride, with ethylene glycol and oxidation to 2- (5-cholestren-3-β-oxy) -1-acetic acid, 2,3,4-Tetra-O-trimethylsilyl-β-D-glucopyranose was esterified with condensing agent DCC and deprotected with trifluoroacetic acid in tetrahydrofuran to obtain the target ligand. Results A glucose cholestatic conjugate was synthesized. Conclusion The target compounds and important intermediates were confirmed by IR, 1HNMR, MS and so on.