摘要
目的改进3-(3-氯丙基)-1,3,4,5-四氢-7,8-二甲氧基-2H-3-苯并氮杂-2-酮的合成工艺。方法以3,4-二甲氧基苯乙酸为原料,先后经氯代、酰化、环和、取代和氢化等反应合成目标化合物。结果与结论改进后的方法操作简单,易于纯化,试剂价廉易得,适合于工业化生产,总产率由44%提高到48%。
OBJECTIVE To improve the process of synthesis of 3 - （3 - chloropropyl） - 1,3 - dihydro - 7,8 - dimethoxyl - 2H - 3 - benzazepin -2 - one. METHODS The target compound I was synthesized from 3,4 - dimethox - phenylacetyl chloride Ⅲ which consisted of chloration, acylation, condensation, substitution and hydrolysis reaction. RESULTS and CONCLUSION The improved synthetic method is convenient and might be applied for the industrial manufacture with the increased overall yield from 44% to 48%.
出处
《华西药学杂志》
CAS
CSCD
北大核心
2009年第5期471-472,共2页
West China Journal of Pharmaceutical Sciences
基金
国家自然科学基金资助项目(批准号:29972013)
关键词
伊伐布雷定
心绞痛
中间体
合成
Ivabradine
Angina pectoris
Intermediates
Synthesis
