新型抗心绞痛药雷诺嗪的合成研究

Synthesis of a novel antianginal agent ranolazine

目的合成新型抗心绞痛药雷诺嗪。方法以邻甲氧基苯酚、环氧氯丙烷、2,6-二甲基苯胺、哌嗪为原料,采用常规的化学合成法。结果通过优化条件以较高的收率合成雷诺嗪二盐酸盐。结论用元素分析、质谱、氢谱、碳谱等鉴定了目标物的结构。优化了反应条件,简化了后处理过程,为进一步工业生产和临床应用打下基础。

Aim To synthesize ranolazine, a novel antianginal agent which inhibits partial fatty acid oxidation, reduces myocardical infarct size and cardiac troponin release. Method Exploiting o-methoxyphenol, 2, 6-dimethylaniline, piperazine and epoxychloropropane as starting materials, ranolazine was prepared through a 4-step procedure. Result and Conclusion Ranolazine dihydrochloride was prepared in a good yield. The structure of the target compound was confirmed by MS, 1H-NMR, 13C-NMR spectra and elemental analy-