雷诺嗪的合成

Synthesis of Ranolazine

目的抗心绞痛新药雷诺嗪的合成。方法以2,6-二甲基苯胺为原料,经氯乙酰化,与无水哌嗪缩合,最后与1-(2-甲氧苯氧基)-2,3-环氧丙烷(2)反应制得雷诺嗪。结果合成产物经熔点、红外光谱、核磁共振谱、质谱等确定结构,并改进了中间体1-[(2,6-二甲基苯基)甲酰胺甲基]哌嗪(4)的合成工艺,从而提高了目标产物的纯度和收率。结论本工艺路线方法简单,原料易得,易于工业化生产。

OBJECTIVE To synthesize Ranolazine,anew drug for the treatment of antianginal.METHOD Ranolazine was prepared from 2,6-dimethylaniline by chloacetylation,condensation with piperazine,at last treated with l-(2-methoxyphenoxy)-2,3-epoxypropane(2) to get Ranolazine.RESULTS The structure of Ranolazine was Characterized by the melting point,IR,IHNMR and MS.The preparative of immediate l-[(2,6-dimethylphenyl) aminocarbonylmethyl]piperazine(4) was improved,the purity and the yield of the target compound were increased.CONCLUSION The process can be easily controlled and is suitable for a scale production.