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雷诺嗪的合成 被引量:5

Synthesis of Ranolazine
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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).
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2004年第11期641-642,共2页 Chinese Journal of Pharmaceuticals
关键词 雷诺嗪 抗心绞痛药 合成 ranolazine antianginal drug synthesis
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参考文献3

  • 1Allely MC, Alps BJ. The effects of the novel antianginal compound RS 43285 on myocardial conduction in the anesthetized dog [J]. Br J Pharmacol, 1988, 93 (2) :375-382.
  • 2Kluge AF, Clark RD, Strosberg AM, et al. Cardioselective aryloxy- and arylthio- hydroxypropylene-piperazinyl acetanilides which effect calcium entry [P]. US: 4567264, 1986-01-28; EP: 126449, 1984-11-28. (CA 1985, 102: P166777h)
  • 3Baumgarter HE. Organic Syntheses [M]. Coll Vol V, New York: John Wiley, 1973.88-91.

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