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对 2 去氧 2 ,3 去氢 N 乙酰基神经氨酸 (Neu5Ac2en)的 8 羟基和 9 羟基进行选择性硫酸酯化 ,以比较不同取代位置的硫酸酯基对唾液酸酶抑制活性的影响。采用三苯甲基氯保护 9 羟基后 ,对 8 羟基进行选择性硫酸酯化 ;在 4,7,8 三羟基乙酰化后 ,酸性条件下水解 9 三苯甲基醚 ,对9 羟基进行选择性硫酸酯化。得到 7个结构全新的Neu5Ac2en 8 硫酸酯衍生物、9 硫酸酯衍生物。初步生物活性试验表明 ,这些化合物均具有一定的唾液酸酶抑制活性 ,9 硫酸酯衍生物的酶抑制活性高于 8 硫酸酯衍生物。
Selective sulfation of 8-hydroxyl and 9-hydroxyl groups of 2-deoxy 2, 3-dehydroacetylneuraminic acid (Neu5Ac2en) was performed to compare the effect of sulfate groups at different substitution positions on sialidase inhibitory activity. After the 9 hydroxyl group was protected by trityl chloride, the 8 hydroxyl group was selectively sulfated. After 4,7,8 trihydroxyacetylation, 9 trityl ether was hydrolyzed under acidic condition, and the selectivity to 9 hydroxyl group Sulfurized. Seven new Neu5Ac2en8 sulfate derivatives and nine sulfate derivatives were obtained. Preliminary biological activity tests showed that these compounds have some sialidase inhibitory activity, 9 sulfate ester derivatives inhibitory activity higher than 8 sulfate derivatives.