中国药物化学杂志
中國藥物化學雜誌
중국약물화학잡지
Chinese Journal of Medicinal Chemistry
2003年
3期
159-161
,共3页
张为革%齐平%李春刚%谢寅省%高翔%计志忠
張為革%齊平%李春剛%謝寅省%高翔%計誌忠
장위혁%제평%리춘강%사인성%고상%계지충
药物化学%合成%水解%3-O-去红霉糖红霉素衍生物
藥物化學%閤成%水解%3-O-去紅黴糖紅黴素衍生物
약물화학%합성%수해%3-O-거홍매당홍매소연생물
medicinal chemistry%synthesis%hydrolysis%3-O-descladinosylerythromycin A derivatives
目的开发一种合成酮基内酯和酰基内酯常用中间体3-O-去红霉糖衍生物的新方法.方法红霉素9(E)-(O-烷基)-肟衍生物与对甲基苯磺酸一水合物在DMF中于室温下反应选择性水解红霉素得到相应的3-O-去红霉糖衍生物.结果高收率得到3-O-去红霉糖衍生物并利用MS、13C-NMR、1H-NMR和IR确定了其结构.结论该方法是制备3-O-去红霉糖红霉素衍生物的简捷、有效的新途径.
目的開髮一種閤成酮基內酯和酰基內酯常用中間體3-O-去紅黴糖衍生物的新方法.方法紅黴素9(E)-(O-烷基)-肟衍生物與對甲基苯磺痠一水閤物在DMF中于室溫下反應選擇性水解紅黴素得到相應的3-O-去紅黴糖衍生物.結果高收率得到3-O-去紅黴糖衍生物併利用MS、13C-NMR、1H-NMR和IR確定瞭其結構.結論該方法是製備3-O-去紅黴糖紅黴素衍生物的簡捷、有效的新途徑.
목적개발일충합성동기내지화선기내지상용중간체3-O-거홍매당연생물적신방법.방법홍매소9(E)-(O-완기)-우연생물여대갑기분광산일수합물재DMF중우실온하반응선택성수해홍매소득도상응적3-O-거홍매당연생물.결과고수솔득도3-O-거홍매당연생물병이용MS、13C-NMR、1H-NMR화IR학정료기결구.결론해방법시제비3-O-거홍매당홍매소연생물적간첩、유효적신도경.
Aim To develop a new procedure for the synthesis of 3-O-descladinosylerythromycin A derivatives as very useful synthetic intermediates of ketolides and acylides.Method Selective cleavage of cladinose by treatment of erythromycin A 9(E)-(O-alkyl)-oxime derivatives with p-toluenesulfonic acid monohydrate at room temperature in DMF provided corresponding 3-O-descladinosylerythromycin A derivatives.Results 3-O-descladinosylerythromycin A derivatives were obtained in excellent yields while their structures were characterized by the applications of MS,13C-NMR,1H-NMR and IR.Conclusion The present method was proved to be a more convenient and effective approach to 3-O-descladinosylerythromycin A derivatives.
