A process for the preparation of a 2-chloro- 2-deoxy-mono, di- or oligo-saccharide, comprises reaction of a mono-, di- or oligo-sapqharide derivative having a free hydroxy group in at least 2- position and having the hydroxy group in at least the 1 - and 3- positions protected from chlorination, with sulphuryl chloride in the presence of an organic base in a chlorinated hydrocarbon solvent at a temperature below -40°C to form a chlorosulphate derivative with a chlorosulphate derivative isthen reacted with lithium chloride in the presence of hexamethylphosphoric triamide to replace chlorosulphate groups with chlorine atoms to form a chlorodeoxy derivative, which chlorodeoxy derivative is then freed of unwanted protecting groups.
一种制备 2-
氯-2-脱氧
单糖、
双糖或低聚糖的工艺,包括在有机碱存在下,在
氯化烃溶剂中,在低于-40℃的温度下,使至少在 2-位上具有游离羟基和至少在 1-位和 3-位上具有不被
氯化保护的羟基的
单糖、
双糖或低聚糖衍
生物与
硫酰氯反应,形成
氯代
硫酸酯衍
生物,然后在六甲基三
磷酰胺存在下,使
氯代
硫酸酯衍
生物与
氯化锂反应,用
氯原子取代
氯代
硫酸酯基团,形成
氯代脱氧衍
生物,然后使
氯代脱氧衍
生物摆脱不需要的保护基团。