中国药物化学杂志
中國藥物化學雜誌
중국약물화학잡지
Chinese Journal of Medicinal Chemistry
2008年
6期
429-433
,共5页
周宇%李剑%李建%赵临襄%蒋华良%柳红
週宇%李劍%李建%趙臨襄%蔣華良%柳紅
주우%리검%리건%조림양%장화량%류홍
工艺研究%禽流感%扎那米韦
工藝研究%禽流感%扎那米韋
공예연구%금류감%찰나미위
process research%avian influenza%zanamivir
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-NMR 13C-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%.
目的 研究治療禽流感藥物扎那米韋的閤成工藝.方法 以N-乙酰神經氨痠作為起始原料,經過酯化、酰化、成環、開環、疊氮化、還原、水解及AIMSA取代等8步反應製備扎那米韋.結果與結論 經過對閤成工藝的改進得到瞭目標產物,其結構經1H-NMR 13C-NMR、LR-MS、HR-MS、元素分析和X-晶體衍射予以確證.總收率為10.1%.
목적 연구치료금류감약물찰나미위적합성공예.방법 이N-을선신경안산작위기시원료,경과지화、선화、성배、개배、첩담화、환원、수해급AIMSA취대등8보반응제비찰나미위.결과여결론 경과대합성공예적개진득도료목표산물,기결구경1H-NMR 13C-NMR、LR-MS、HR-MS、원소분석화X-정체연사여이학증.총수솔위10.1%.
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%.
