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【结 构 式】 
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【药物名称】Bifeprunox mesilate, DU-127090 【化学名称】7-[4-(Biphenyl-3-ylmethyl)piperazin-1-yl]benzoxazol-2(3H)-one methanesulfonate 【CA登记号】350992-13-1, 362524-71-8, 350992-10-8 (free base), 197954-51-1 (hydrochloride) 【 分 子 式 】C25H27N3O5S 【 分 子 量 】481.57504 |
【开发单位】Solvay (Originator), Lundbeck (Licensee), Wyeth Pharmaceuticals (Licensee) 【药理作用】Antiparkinsonian Drugs, Antipsychotic Drugs, Extrapyramidal Disorders, Treatment of, NEUROLOGIC DRUGS, PSYCHOPHARMACOLOGIC DRUGS, 5-HT1A Receptor Agonists, Dopamine D2 Antagonists |
合成路线1
The title compound was prepared by alkylation of 7-piperazinylbenzoxazol-2(3H)-one (I) with 3-phenylbenzyl bromide (II) in the presence of diisopropyl ethyl amine and KI in refluxing acetonitrile.
| 【1】 Feenstra, R.W.; et al.; New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D2-receptor and serotonin 5-HT1A-receptor affinities. Bioorg Med Chem Lett 2001, 11, 17, 2345. |
| 【2】 Feenstra, R.W.; Kruse, C.G.; Tulp, M.T.M.; Kuipers, W.; Long, S.K. (Duphar International Research BV); Piperazine and piperidine cpds.. JP 2000507949; US 6225312; WO 9736893 . |
Extended Information