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【结 构 式】 
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【药物名称】Tenilsetam, CAS-997 【化学名称】(±)-3-(2-Thienyl)-2-piperazinone 【CA登记号】86696-86-8 【 分 子 式 】C8H10N2OS 【 分 子 量 】182.2457 |
【开发单位】Aventis Pharma (Originator) 【药理作用】Cognition Disorders, Treatment of, Diabetic Retinopathy, Agents for, ENDOCRINE DRUGS, NEUROLOGIC DRUGS, Treatment of Diabetic Complications, AGE Inhibitors (Maillard's Reaction Inhibitors) |
合成路线1
The cyclization of ethyl 2-(2-thienyl)glyoxylate (I) with ethylenediamine (II) in refluxing ethanol gives 3-(2-thienyl)-1,2,5,6-tetrahydropyrazin-2-one (III), which is reduced with H2 over Raney Nickel (RaNi) in hot ethanol at 50 bar.
| 【1】 Beyerle, R.; Bender, H.; Schindler, U.; Nitz, R.-E.; Martorana, P.A. (Cassella AG); Novel piperazinones, their preparation and use. DE 3132882; US 4598079 . |
| 【2】 Tilford, C.H.; Carr, A.A. Jr.; Kuhn, W.L. (Aventis Pharmaceuticals, Inc.); Substd. 5,6-dihydro-2(1H)-pyrazinones. US 3056784 . |
| 【3】 Castaner, J.; Prous, J.; Telnisetam. Drugs Fut 1988, 13, 2, 130. |
Extended Information