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【结 构 式】 
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【药物名称】VN-2222 【化学名称】1-(Benzothien-3-yl)-3-[4-(2-methoxyphenyl)-1-piperazinyl]-1-propanol hydrochloride 【CA登记号】 【 分 子 式 】C22H27ClN2O2S 【 分 子 量 】418.98969 |
【开发单位】Vita (Originator) 【药理作用】Antidepressants, Mood Disorders, Treatment of, PSYCHOPHARMACOLOGIC DRUGS, 5-HT Reuptake Inhibitors, 5-HT1A Partial Agonists |
合成路线1
Mannich reaction of N-(2-methoxyphenyl)piperazine (I) with 3-acetylbenzothiophene (II) in the presence of paraformaldehyde and HCl in refluxing EtOH leads to the piperazinyl propanone (III). Subsequent keto group reduction with NaBH4 gives the target alcohol.
| 【2】 Bosch Rovira, A.; Roca Acin, J.; Monge Vega, A.; Del Rio Zambrana, J.; Palop Cubillo, J.A.; Lasheras Aldaz, B.; Del Castillo Nieto, J.C. (Laboratorios Vita, SA); Cpds. derived from thiophene and benzothiophene, and related utilisation and compsn.. EP 1008594; ES 2128266; JP 2002511883; US 6262056; WO 9902516 . |
| 【1】 Oficialdegui, A.-M.; Martínez-Esparza, J.; Pérez-Sailanes, S.; et al.; New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants. J Med Chem 2001, 44, 3, 418. |
Extended Information