N-去甲基十二元环红霉素衍生物的直接合成(英文)  

Straightforward synthesis of the N-monodemethylated 12-membered-ring erythromycin derivative

作　　者：张为革[1] 王虹[1] 任岩[1] 金龙[1] 包凯[1] 林金光[1] 姚新生[2] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016 [2]清华大学研究院中药及天然药物研究中心,广东深圳518057

出　　处：《中国药物化学杂志》2003年第6期342-344,共3页Chinese Journal of Medicinal Chemistry

基　　金：TheprojectwassupportedbyShenyangBureauofScience&Technology ( 2 0 0 12 2 8- 0 9- 0 5&0 2Z0 1060)andLiaoningBureauofScience&Technology ( 2 0 0 2 10 2 8)

摘　　要：目的开发一种用于合成具有抗炎活性红霉素衍生物的中间体———N 去甲基十二元环红霉素衍生物的直接方法。方法 8,9 脱水红霉素 6 ,9 半缩酮与碘在碱性溶剂中反应得到相应的N 去甲基十二元环红霉素衍生物。结果以6 6 %的收率得到N 去甲基十二元环红霉素衍生物并利用质谱、核磁共振碳谱和红外光谱确定了其结构。结论该方法是制备N 去甲基十二元环红霉素衍生物的方便。Aim To develop a straightforward method for the synthesis of N monodemethylated 12 membered ring erythromycin derivative as a useful synthetic intermediate of new erythromycin derivatives with antiinflammatory activity.Method Treatment of 8,9 anhydroerythromycin 6,9 hemiketal with iodine in the alkaline solution provided corresponding N monodemethylated 12 membered ring erythromycin derivative.Results The N monodemethylated 12 membered ring erythromycin derivative was obtained in 66% yield while its structure was characterized by the applications of MS, 13 C NMR and IR.Conclusion The present method was proved to be a more convenient and effective approach to the N monodemethylated 12 membered ring erythromycin derivative.

关 键 词：药物化学 制备 化学合成 N-去甲基十二元环红霉素衍生物 

分 类 号：R914[医药卫生—药物化学]