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【结 构 式】 
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【药物名称】Org-13011 【化学名称】1-[4-[4-[4-(Trifluoromethyl)pyridin-2-yl]piperazin-1-yl]butyl]pyrrolidin-2-one fumarate 【CA登记号】 【 分 子 式 】C22H29F3N4O5 【 分 子 量 】486.49543 |
【开发单位】Akzo Nobel (Originator), Organon (Originator) 【药理作用】Antidepressants, Antipsychotic Drugs, Mood Disorders, Treatment of, PSYCHOPHARMACOLOGIC DRUGS, 5-HT1A Receptor Agonists |
合成路线1
Alkylation of 2-pyrrolidinone (I) with 1,4-dibromobutane (II) in the presence of KOH and tetraethylammonium bromide gave the N-(4-bromobutyl)pyrrolidinone (III). This was condensed with 1-[4-(trifluoromethyl)-2-pyridinyl]piperazine (IV) in the presence of Na2CO3 to produce the target disubstituted piperazine, which was then converted to the corresponding fumarate salt.
| 【1】 Carlier, P.; Combourieu, M.; Poisson, C.; Monteil, A.J.-C. (Akzo Nobel N.V.); 4-[4- or 6-(Trifluoromethyl-2-pyridinyl)]-1-piperazinyl-alkyl substd. lactams. EP 0482696; JP 1992282379; US 5180726 . |
Extended Information