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项目整合精选>>>Donepezil hydrochloride, BNAG, E-2020, Eranz, Memorit, Memac, Aricept
Donepezil hydrochloride, BNAG, E-2020, Eranz, Memorit, Memac, Aricept
盐酸多奈哌齐Chemical Name: (?-1-Benzyl-4-(5,6-dimethoxy-1-oxoindan-2-ylmethyl)piperidine hydrochloride; (?-2-(1-Benzylpiperidin-4-ylmethyl)-5,6-dimethoxyindan-1-one hydrochloride
CAS No. 120011-70-3, 123958-79-2 ([2-14C]-labeled), 142057-77-0 (deleted CAS), 120014-06-4 (free base)
项目整合开发状态: Launched-1997
项目研究机构: Eisai (Originator), National Institute of Mental Health (Not Determined), Bracco (Licensee), Pfizer (Licensee)
合成路线:The condensation of 5,6-dimethoxy-1-indanone (I) with 1-benzylpiperidine-4-carboxaldehyde (II) by means of butyllithium and diisopropylamine in THF gives 1-benzyl-4-(5,6-dimethoxy-1-oxoindan-2-ylidenemethyl)piperidine (III),which is reduced with H2 over Pd/C in THF and treated with HCl in dichloromethane - ethyl acetate.
📌 参考资料/链接：
参考文献标题:Cyclic amine cpd.,its use and pharmaceutical compsns.comprising it
文献作者:Sugimoto,H.; Tsuchiya,Y.; Higurashi,K.; Karibe,N.; Iimura,Y.; Sasaki,A.; Yamanashi,Y.; Ogura,H.; Araki,S.; Kosasa,T.; Kusota,A.; Kozasa,M.; Yamatsu,K.(Eisai Co.,Ltd.)
参考来源:AU 8818216; EP 0296560; EP 0673927; EP 0742207; JP 1989079151; JP 1998067739; US 4895841; US 5100901
📄 详细内容
合成路线:The condensation of 5,6-dimethoxy-1-indanone (I) with 1-benzylpiperidine-4-carboxaldehyde (II) by means of butyllithium and diisopropylamine in THF gives 1-benzyl-4-(5,6-dimethoxy-1-oxoindan-2-ylidenemethyl)piperidine (III),which is reduced with H2 over Pd/C in THF and treated with HCl in dichloromethane - ethyl acetate.
参考文献标题:Synthesis of 1-benzyl-4-[(5,6-dimethoxy[2-14C]-1-indanon)-2-yl]methylpiperidine hydrochloride (E-2020-14C)
文献作者:Sugimoto,H.; Mishima,M.; Iimura,Y.
参考来源:J Label Compd Radiopharm 1989,27(7),835-9
合成路线:The condensation of 5,6-dimethoxy-1-indanone (I) with 1-benzylpiperidine-4-carboxaldehyde (II) by means of butyllithium and diisopropylamine in THF gives 1-benzyl-4-(5,6-dimethoxy-1-oxoindan-2-ylidenemethyl)piperidine (III),which is reduced with H2 over Pd/C in THF and treated with HCl in dichloromethane - ethyl acetate.
参考文献标题:E-2020
文献作者:Castar,J.; Prous,J.
参考来源:Drugs Fut 1991,16(1),16
合成路线:11C-Labeled donepezil was prepared by methylation of 2-(1-benzylpiperidin-4-ylmethyl)-6-hydroxy-5-methoxyindan-1-one (I) with 11CH3I by means of tetrabutylammonium hydroxide in DMF.
参考文献标题:Synthesis of 1-benzyl-4-[(5,[C-11]6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine: A promising ligand for visualisation of acetylcholine esterase by PET
文献作者:Santens,P.; DeReuck,J.; Dierckx,R.A.; Siegers,G.; Vermeirsch,H.; De Vos,F.
参考来源:J Label Compd Radiopharm 2000,43(6),595
产品链接: CAS No. 120011-70-3›› 产品链接: CAS No.142057-77-0››