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项目整合精选>>>Aniracetam, Ro-13-5057, Reset, Ampamet, Sarpul, Draganon
Aniracetam, Ro-13-5057, Reset, Ampamet, Sarpul, Draganon
阿尼西坦Chemical Name: 1-p-Anisoyl-2-pyrrolidinone; 1-(4-Methoxybenzoyl)pyrrolidin-2-one
CAS No. 72432-10-1
项目整合开发状态: Launched-1993
项目研究机构: Roche (Originator), Biomedica Foscama (Licensee), Menarini (Licensee), Toyama (Licensee)
合成路线:The silylation of 4-acetoxy-2-pyrrolidone (I) with trimethylchlorosilane (II) by means of triethyl amine in THF gives the corresponding N-trimethylsilyl derivative (III),which is condensed with 4-methoxybenzoyl chloride (IV) by means of NaHCO3 in THF yielding 1-(4-methoxybenzoyl)pyrrolin-2-one (V).Finally,this compound is reduced with H2 over Pd/C in ethyl acetate.
合成路线:The condensation of 4-aminobutyric acid (VI) with acid chloride (IV) by means of NaOH in water gives 4-(4-methoxybenzoylamino)butyric acid (VII),which is then cyclized by means of P2O5 in phosphoric acid.
合成路线:The condensation of 6-methoxy-2-naphthaldehyde (I) with acetone by means of NaOH in water gives 4-(6-methoxy-2-naphtyl)-3-buten-2-one (II),which is reduced with H2 over Pd/C in ethyl acetate.
📌 参考资料/链接:
参考文献标题:1-(p-Methoxy-p-hydroxy,and p-benzyloxybenzoyl)-2-pyrrolidinones
文献作者:Kyburz,E.; Aschwanden,W.(F.Hoffmann-La Roche AG)
参考来源:DD 141828; EP 0005143; EP 0044088; ES 477587; ES 483756; JP 54117468
📄 详细内容
合成路线:By reaction of 2-pyrrolidinone (I) with p-methoxybenzoyl chloride (II) by means of triethylamine in ether or sodium hydride in DMF.
参考文献标题:Aniracetam
文献作者:Blancafort,P.; Serradell,M.N.; Mealy,N.E.; Leeson,P.A.; Castar,J.
参考来源:Drugs Fut 1981,6(3),127
合成路线:By reaction of 2-pyrrolidinone (I) with p-methoxybenzoyl chloride (II) by means of triethylamine in ether or sodium hydride in DMF.
参考文献标题:1-(P-Methoxy,p-hydroxy and p-benzyloxybenzoyl)-2-pyrrolidinones
文献作者:Kyburz,E.; Aschwanden,W.
参考来源:EP 0005143; JP 54117468; US 4369139
产品链接: CAS No. 72432-10-1››