雷诺嗪的合成  

Synthesis of Ranolazine

作　　者：陆文超[1] 李瑛琦[1] 赵祥麟[1] 郭春[1] 周凯 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016 [2]东北制药总厂,辽宁沈阳110024

出　　处：《中国医药工业杂志》2004年第11期641-642,共2页Chinese Journal of Pharmaceuticals

摘　　要：2,6-二甲苯胺加氯乙酰氯制得酰胺后与哌嗪反应得N-(2,6-二甲苯基)-2-(1-哌嗪基)乙酰胺,其与由邻甲氧基苯酚和环氧氯丙烷反应得到的2-(2-甲氧苯氧基甲基)环氧乙烷反应制得抗心绞痛药雷诺嗪,总收率51%(以2,6-二甲苯胺计)。Ranolazine was synthesized from 2,6-dimethylaniline and 2-chloroacetylchloride by amidation andsubsequent condensation with piperazine to give N-(2,6-dimethylphenyl)-2-(1-piperazinyl)acetamide, which subjected tocondensation with 2-(2-methoxyphenoxy)oxirane prepared by condensation of 2-methoxyphenol and epichlorohydrin withan overall yield of 51%(based on 2,6-dimethylaniline).

关 键 词：雷诺嗪 抗心绞痛药 合成 

分 类 号：R971.3[医药卫生—药品]