扎那米韦的合成工艺研究(英文)  

Improved synthesis of resveratrol

作　　者：周宇[1,2] 李剑[3] 李建[1] 赵临襄[2] 蒋华良[1,3] 柳红[1] 

机构地区：[1]中国科学院上海药物研究所药物发现与设计中心,上海201203 [2]沈阳药科大学制药工程学院,辽宁沈阳110016 [3]华东理工大学药学院,上海200237

出　　处：《中国药物化学杂志》2008年第6期429-433,共5页Chinese Journal of Medicinal Chemistry

基　　金：National Key Technology R&D Programof China(Grant 2006BAI01B02);the Key Project for New Drug Re-search from CAS,and the 863 Hi-Tech Program(Grants 2006AA020602,2006AA02Z336)

摘　　要：目的研究治疗禽流感药物扎那米韦的合成工艺。方法以N-乙酰神经氨酸作为起始原料,经过酯化、酰化、成环、开环、叠氮化、还原、水解及AIMSA取代等8步反应制备扎那米韦。结果与结论经过对合成工艺的改进得到了目标产物,其结构经1H-NMR1、3C-NMR、LR-MS、HR-MS、元素分析和X-晶体衍射予以确证。总收率为10.1%。Aim To develop the practical synthetic route of zanamivir, a drug for AIV treatment. Methods Zanamivir was synthesized by using N-acetylneuraminic acid as the starting material, through an eight-step process including esterification, acylation, cyclization, ring-opening, azide substitution, reduction, and hydrolysis followed by reaction with aminoiminomethanesulfonic acid （AIMSA）. Results and conclusion The target compound was synthesized by an improved route, and was verified by ^1H-NMR, ^13C-NMR, LR-MS, HR-MS, elemental analysis and X-ray. The total yield is 10.1%.

关 键 词：工艺研究 禽流感 扎那米韦 

分 类 号：TQ463[化学工程—制药化工]