目的 對(duì)磺達(dá)肝癸鈉中單糖中間體的合成工藝進(jìn)行改進(jìn)研究。方法 以D-氨基葡萄糖為起始原料,經(jīng)甲苷反應(yīng)、芐基化反應(yīng)得到單糖中間體。結(jié)果 得到了α構(gòu)型磺達(dá)肝癸鈉甲苷單糖片段產(chǎn)物,HPLC檢測質(zhì)量分?jǐn)?shù)可達(dá)98%以上,總收率為41.2%。結(jié)論 磺達(dá)肝癸鈉甲苷單糖中間體的合成工藝可簡化操作,降低成本,提高安全性,方便生產(chǎn)。

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.

天津市科技計(jì)劃項(xiàng)目(13ZCZDSY00600)