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经由路易斯酸BF_3·Et_2O催化全乙酰化糖缀合物合成反应中,只有纯β构型全乙酰化保护糖因其反应中邻基参与效应可以参与反应过程.基于此种机理,为了能得到更多纯β构型全乙酰化保护糖以提高总路线的产率,需要探索出高效糖全乙酰化保护反应.通过对所待选的众多非金属绿色催化剂进行对比,无水醋酸钠因其产率高、构型选择性好被证实是最为理想的糖全乙酰化催化剂.在得到糖全乙酰化产物后,由于不同构型的溶解能力不同,对其进行重结晶可以得到单一β构型的糖全乙酰化产物.基于以上反应,找到了一条高效简便高产率且得到纯β构型全乙酰化保护糖缀合物的合成路线.
Through the Lewis acid BF_3 · Et_2O catalyzed synthesis of acetyl-glycoconjugates, only the pure β-acetyl-protected glycoconjugates can participate in the reaction process due to the participation of the adjacent groups in the reaction.Based on this mechanism, in order to obtain more In order to improve the yield of the total route, it is necessary to explore the efficient acetyl-protection reaction.Through the comparison of many non-metallic green catalysts to be selected, the yield of anhydrous sodium acetate due to its yield High selectivity and good configuration selectivity proved to be the most ideal sugar holoacetylation catalyst.After obtaining the sugar acetylation product, due to the different dissolving ability of different configurations, it can be obtained by recrystallization of a single β-configuration sugar Based on the above reaction, a synthetic route was found to be simple and efficient with high yield and yielding a pure β-configuration peracetylated protective glycoconjugate.