肾靶向脂质体配体巯基葡萄糖-胆甾偶联物的设计与合成  

Synthesis of sulfhydryl glucose-cholesterol as ligand for kidney targeting liposomes

作　　者：肖湘[1] 樊维[1] 蒋庆琳[1] 吴勇[1] 海俐[1] 

机构地区：[1]四川大学华西药学院,四川成都610041

出　　处：《华西药学杂志》2011年第3期221-223,共3页West China Journal of Pharmaceutical Sciences

摘　　要：目的设计并合成一种新型的肾靶向脂质体配体巯基葡萄糖-胆固醇偶联物。方法胆固醇与对甲苯磺酰氯成酯后与癸二醇取代,甲磺酰氯磺酰化制得6-(5-胆甾烯-3-氧基)-1-甲烷磺酰氧基癸烷,再与1,2,3,4-四-O-乙酰基-1-巯基-吡喃葡萄糖成醚后由甲醇钠脱保护后得到目标配体。结果成功合成一个胆甾巯基葡萄糖偶联物。结论目标化合物已经IR、1HNMR、MS确证。OBJECTIVE To design and synthesize an novel glucose-cholesterol as kidney targeting ligand for liposome.METHODS The title compound was synthesized from cholesterol and compound III was afforded by tosylation,substitution and sulfonylation of the starting material.The coupling reaction of intermediate Ⅲ and 1,2,3,4-tetra-O-acetyl-1-sulfhydryl glucopyranose with DIPEA and potassium iodide furnished compound Ⅴ,which was finally deprotected by sodium methoxide to obtain the title compound L.RESULTS The title compound was designed and synthesized.CONCLUSION The chemical structure of the target compound and intermedium were confirmed by IR,1HNMR and MS.

关 键 词：肾靶向 脂质体配体 胆固醇 巯基葡萄糖 合成 

分 类 号：R914[医药卫生—药物化学]