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LIU Bao, WU Kai, SUN Ruiqin, JIANG Yuwei, ZHANG Xiaoqing. Practical synthesis of tofisopam[J]. Journal of China Pharmaceutical University, 2014, 45(6): 671-673. DOI: 10.11665/j.issn.1000-5048.20140609
Citation: LIU Bao, WU Kai, SUN Ruiqin, JIANG Yuwei, ZHANG Xiaoqing. Practical synthesis of tofisopam[J]. Journal of China Pharmaceutical University, 2014, 45(6): 671-673. DOI: 10.11665/j.issn.1000-5048.20140609

Practical synthesis of tofisopam

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  • This paper deals with the development of a practical process for tofisopam( 1 ). The target product 1 was synthesized from commercially available isoeugenenyl methyl ether( 2 )in a two-step process with an overall yield of 48% via polymerization, oxidation(56% yield)and cyclization with Hydrazine hydrate(87% yield). The intermediates and the target product were characterized by 1H NMR, 13C NMR and ESI-MS. This synthetic process of tofisopam is featured with robustness, high yielding in almost every step, ease of operation, as well as green chemistry, and thus should be amenable to large-scale production.
  • [1]
    Kucharik R,Harris H.Block sensitivity to leukotrienes;inflammatory bowel disorders;psoriasis;antiarthritic agents:US,20040138209[P].2003-12-03[2004-07-15] .
    [2]
    Molnárnésamu E,Simig TH.Process for the preparation of 3-[2-(3,4-dimethoxybenzoyl)-4,5-dimethoxyphenyl]-pentan-2-one:WO,2004054952[P].2003-12-16[2004-07-01] .
    [3]
    Harris HW,Kucharik RF.Treatment of irritable bowel syndrome and nonulcer dyspepsia with substituted 2,3-benzodiazepines:US,6638928[P].2002-12-03[2003-10-28] .
    [4]
    Zhang KH,Zhang YF,Hu WQ.A process for preparing a tofisopan intermediate:CN,101823945[P].2009-03-06[2010-09-08] .
    [5]
    Bernard P.Phosphodiesterase inhibitors:US,20070161628[P].2006-11-20[2007- 07-12] .
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