磺达肝癸钠中间体——1,2,4,6-氧-乙酰基-3-氧-苄基-L-艾杜糖的合成

Synthesis of 1,2,4,6-O-Acetyl-3-O-benzyl-L-idonic

以1,2:5,6-氧-二异亚丙基-α-D-呋喃葡萄糖为原料,依次通过苄基保护、脱保护、甲磺酰化、酯交换、环氧化、水解重排并乙酰化得到标题化合物,总产率68.2%。该方法操作简便,适宜工业化。

Starting from 1,2： 5,6-Di-O-isopropylidene-alpha-D-glucofuranose,the fondaparinux sodium intermediate compound,1,2,4,6-O-acetyl-3-O-benzyl-L-idonic was obtained by seven steps reaction such as benzyl protection,deprotection,mesylation,epoxidation,transesterification,hydrolysis rearrangement,and acetylation successively. The total yield was 68. 2%. The process is simple and suitable for industrial production.