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详细研究了N-乙酰基-5-N,4-O-噁唑烷酮保护的唾液酸对甲基苯硫苷给体1与四种苄基或苯甲酰基保护的半乳糖甲苷二醇的唾液酸化反应,以较高的产率(72%～89%)得到了相应的唾液酸化产物,α/β=(1.6～2.0)∶1.在此基础上,以乳糖为原料通过7步反应以19%的总产率制得了2,3,6,2’,6’-五-O-苯甲酰基-β-乳糖甲苷17,使用唾液酸给体1将化合物17唾液酸化,成功地得到神经节苷脂GM3三糖甲苷衍生物18,产率68%,α/β=1.6∶1.
The effects of N-acetyl-5-N, 4-O-oxazolidinone protected sialic acid p-methylthiophenyl glycoside donor 1 and four benzyl or benzoyl protected galactosidyl glycosides Sialylation reaction, the corresponding sialylated product was obtained in higher yield (72% ~ 89%), α / β = (1.6 ~ 2.0): 1.On this basis, Reaction 2,3,6,2 ’, 6’-Penta-O-Benzoyl-β-Lactoside 17 was prepared in 19% overall yield and Compound 17 was sialylated using Sialic Acid Donor 1 Ganglioside GM3 trisaccharide glycoside derivative 18 was obtained in a 68% yield with α / β = 1.6: 1.