Synthetic method of eletriptan intermediate 4-nitrophenyl-2-(4-benzenesulfonyl hydrazide)ethane

• Main Authors: GAO LINGFENG, LI WEI, ZHENG GENGXIU, CUI ZHAOXIN, GU HAIYANG, YAO TIANHUI
• Format: Patent
• Language: Chinese; English
• Published: 26.01.2018
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; METALLURGY; ORGANIC CHEMISTRY

The invention discloses a synthetic method of eletriptan intermediate 4-nitrophenyl-2-(4-benzenesulfonyl hydrazide)ethane. According to the synthetic method, 4-nitrostyrene and benzenesulfonyl hydrazide are taken as raw materials, distilled water is taken as a solvent, heating reaction is carried out under acidic conditions, and 4-nitrophenyl-2-(4-benzenesulfonyl hydrazide)ethane is obtained via one-step reaction. The synthetic method is capable of obtaining eletriptan important intermediate 4-nitrophenyl-2-(4-benzenesulfonyl hydrazide)ethane, yield is higher than 90%, purity is higher than 95%, the raw materials are cheap and easily available, operation is simple, side products are few, and the synthetic method is convenient for industrialized production. 本发明公开了种依来曲普坦中间体4-硝基苯基-2-(4-苯磺酰肼)乙烷的合成方法。以对硝基苯乙烯与苯磺酰肼为原料，蒸馏水为溶剂，在酸性条件下加热，步反应生成4-硝基苯基-2-(4-苯磺酰肼)乙烷。该方法经步反应即可得到依来曲普坦的重要中间体4-硝基苯基-2-(4-苯磺酰肼)乙烷，收率达90%以上，纯度达95%以上，该方法原料便宜易得，操作简便，副产物少，易于工业化生产。