Abstract: 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.