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Manufacturing methods and new oligosaccharide of oligosaccharides and pharmaceutical compositions containing it

机译:寡糖的制备方法和新的寡糖以及含有该寡糖的药物组合物

摘要

PROBLEM TO BE SOLVED: To readily obtain the subject compound containing a galactose residue at a reduction end group by subjecting a protected hydroxyl group and a protected amino group in glucosamine and a protected hydroxyl group in galactose to glucoside bond reaction. ;SOLUTION: A monosaccharide of formula I (R1 and R2 are each an aralkyl; R3 is an acyl or silyl; R4 is an amino-protecting group; R5 is an eliminable group) and a monosaccharide of formula II (R6 and R8 are each an aralkyl; R7 is an acyl or silyl; R9 is an aralkyl, 6-O-sulfated N-acetylglucosamine residue, an alkyl, a glycerol residue, or the like; Z is O or NHCO) are subjected to glycoside bond reaction to give an oligosaccharide of formula III (R10 and R11 are each H, an SO3M (M is proton or a monofunctional cation); Ac is acetyl; R12 is H, 6-O-sulfated N-acetylglucosamine residue; an alkyl, a glycerol residue, or the like). A part of the oligosaccharide of formula III is useful as an antiallergic agent or an antiinflammatory agent.;COPYRIGHT: (C)2000,JPO
机译:解决的问题:通过使葡糖胺中的被保护的羟基和被保护的氨基以及半乳糖中的被保护的羟基经受葡糖苷键反应,容易地获得在还原端基上包含半乳糖残基的主题化合物。 ;解决方案:式I的单糖(R1和R2各自为芳烷基; R3为酰基或甲硅烷基; R4为氨基保护基; R5为可消除基团)和式II的单糖(R6和R8各自为使芳烷基; R7为酰基或甲硅烷基; R9为芳烷基,6-O-硫酸化的N-乙酰基葡糖胺残基,烷基,甘油残基等; Z为O或NHCO)进行糖苷键反应以得到式III的寡糖(R 10和R 11各自为H,SO 3 M(M为质子或单官能阳离子); Ac为乙酰基; R 12为H,6-O-硫酸化的N-乙酰基葡糖胺残基;烷基,甘油残基,等)。式III的低聚糖的一部分可用作抗过敏剂或抗炎剂。;版权所有:(C)2000,JPO

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