[关键词]
[摘要]
目的 对磺达肝癸钠中单糖中间体的合成工艺进行改进研究。方法 以D-氨基葡萄糖为起始原料,经甲苷反应、苄基化反应得到单糖中间体。结果 得到了α构型磺达肝癸钠甲苷单糖片段产物,HPLC检测质量分数可达98%以上,总收率为41.2%。结论 磺达肝癸钠甲苷单糖中间体的合成工艺可简化操作,降低成本,提高安全性,方便生产。
[Key word]
[Abstract]
Objective To study the improved method for synthesis of methyl glucosamine intermediate of fondaparinux sodium. Methods D-Glucosamine was used as starting material to synthesize the target compound by methyl glycosylation and benzylation. Results The methyl α-glucosamine intermediate of fondaparinux sodium was synthesized. The purity reaches above 98% by HPLC, and the total yield was 41.2%. Conclusion The synthetic technology of methyl glucosamine intermediate of fondaparinux sodium can simplify the operation, reduce the cost, improve the safety, and is convenient for production.
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[基金项目]
天津市科技计划项目(13ZCZDSY00600)