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树脂糖苷Albinoside III是一种良好的多药耐药外排泵抑制剂,本文探索了高效构建树脂糖苷中喹诺糖模块的方法。从D-葡萄糖硫苷出发,采用一锅法,经4步反应构建了D-喹诺糖模块A,总收率58.4%；从4,6-位苄叉保护的D-葡萄糖硫苷出发,通过3-位选择性的PMB保护,经5步反应构建了正交保护的D-喹诺糖模块E,总收率28.5%。该合成路线中涉及8个新化合物,其结构经1H NMR,13C NMR和HR-MS(ESI)表征。“,”Resign glycoside albinoside III is a good multi-resistant efflux pump inhibitor. The efficient method to synthesize the quinoside building blocks of Albinoside III was reported. The quinoside build-ing block A was synthesized from p-tolyl-1-thio-β-D-glucopyranoside through one-pot strategy by four step reactions in total yield of 58 . 4%. The quinoside building block E was synthesized from p-methyl-phenyl-4,6-O-benzylidene-1-thio-β-D-glucopyranoside through regioselective PMB protection by five step reactions in total yield of 28. 5%. Eight novel compounds were involved in the synthetic route. The structures were characterized by 1 H NMR, 13 C NMR and HR-MS( ESI) .