7,8-二甲氧基-3-(3-碘丙基)-1,3-二氢-2H-3-苯并氮杂-2-酮的制备  

Preparation of 7,8-dimethoxy-3-(3-iodopropyl)-1,3-dihydro-2H-3-benzazepin-2-one

作　　者：刘燕平[1] 黄昕明[1] 王德才[1] 

机构地区：[1]南京工业大学制药与生命科学学院,江苏南京210009

出　　处：《华西药学杂志》2008年第3期267-268,共2页West China Journal of Pharmaceutical Sciences

摘　　要：目的合成抗心绞痛的新药伊伐布雷定的关键中间体7,8-二甲氧基-3-(3-碘丙基)-1,3-二氢-2H-3-苯并氮杂--2-酮。方法以3,4-二甲氧基苯乙酸为原料,经卤化、酰化、环合、烷基化、碘取代等反应制得目标化合物。结果五步反应总收率为63.6%,产物经MS1、HNMR确证结构。结论所用工艺路线具有原料易得、操作简便、收率较高的特点,适用于该中间体的放大制备。OBJECTIVE To synthesize 7,8-dimethoxy-3-(3-iodopropyl)-1,3-dihydro-2H-3-benzazepin-2-one,a key intermediate of Ivabradine(a new antianginal drug).METHODS The target compound was synthesized from 3,4-dimethoxyphenylacetic acid via halogenation,acylation,cyclization,alkylation and iodine substitution reaction.RESULTS Chemical structure of compounds was confirmed by MS and 1HNMR and overall yield was 63.6%.CONCLUCION The materials are available and the procedures are manipulated easily which make the route pra...

关 键 词：7 8-二甲氧基-3-(3-碘丙基)-1 3-二氢-2H-3-苯并氮杂-2-酮 伊伐布雷定 心绞痛 中间体 制备 

分 类 号：R94[医药卫生—药剂学]