目的 設(shè)計(jì)并合成磺達(dá)肝癸鈉的二糖中間體。方法 以β-1,2,3,4,6-五乙?；咸烟菫槠鹗荚? 經(jīng)硫化、芐基化、TEMPO氧化、溴化等反應(yīng)得到葡萄糖醛酸供體E;以3,4,6-三乙酰-D-葡萄糖烯為起始原料, 經(jīng)碘化、疊氮化等反應(yīng)得到內(nèi)醚糖受體F;單糖供體E與受體F經(jīng)偶聯(lián)反應(yīng)得到全保護(hù)二糖EF。結(jié)果 合成了目標(biāo)化合物, 并利用¹H-NMR和MS確證了結(jié)構(gòu);HPLC歸一化法測得質(zhì)量分?jǐn)?shù)為99.01%, 目標(biāo)化合物的總收率為11.1%。結(jié)論 磺達(dá)肝癸鈉二糖中間體的合成可以為磺達(dá)肝癸鈉和其他多糖的合成提供重要的中間體原料。

Objective To design and synthesize disaccharide intermediate of fondaparinux sodium. Methods β-D-(+)-Glucose pentaacetate was used as starting material to synthesize the donor compound E by sulfuration, benzylation, TEMPO oxidization and bromination reactions; 1,5-Anhydro-2-deoxy-D-arabino-hex-1-enitol 3,4,6-tri-O-acetyl ether was used to synthesize the receptor compound F by iodization and azidation reactions; And the fully protected disaccharide EF was used to synthesize by coupled reaction. Results The target compound was synthesized and characterized by 1H-NMR and MS. And the purity detected by HPLC was 99.01%. The total yield of the synthetic route was 11.1%. Conclusion Synthesis of disaccharide intermediate of fondaparinux sodium provides important intermediate material for synthesis of fondaparinux sodium and other polysaccharides.