Practical synthesis of tofisopam

LIU Bao; WU Kai; SUN Ruiqin; JIANG Yuwei; ZHANG Xiaoqing

doi:10.11665/j.issn.1000-5048.20140609

Journal of China Pharmaceutical University > 2014 > 45(6): 671-673. > DOI: 10.11665/j.issn.1000-5048.20140609

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

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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.
- tofisopam,
- synthetic process,
- antidepressant agent

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