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为了控制磺达肝癸钠的质量,合成了中间体全保护戊糖(1)的两个异构体(1a,1b)。以含有葡萄糖醛酸和内醚糖的二糖为起始原料,脱氯乙酰基得到受体二糖,与单糖供体偶联得到三糖,开环、氨解、活化得到三糖供体,与还原端二糖受体偶联得全保护戊糖1(5个糖苷键构型次序为?-?-?-?-?)及其2个异构体1a(?-?-?-?-??和1b(?-?-?-?-?)。并经1H NMR和ESI-MS等确证了结构。
In order to control the quality of fondaparinux, two isomers (1a, 1b) of pentose (1) were fully protected. Disaccharide containing glucuronic acid and lactose as a starting material, dechlorination acetyl acceptor disaccharide, and monosaccharide donor coupling to give trisaccharide, ring opening, ammonolysis, activated trisaccharide donor , And the reductive disaccharide acceptor was coupled to protect pentose 1 (5 glycosidic bond order -? -? -? -?) And its two isomers 1a (? -? -? - And 1b (? -? -? -? -?). The structures were confirmed by 1H NMR and ESI-MS.