CAS: 844694-84-4; 1-Benzyl-4-((5,6-Dimethoxy-2,3-Dihydro-1H-Inden-2-yl)Methyl)Piperidine

上下游产品

5,6-dimethoxy-2-[(4-piperidinyl)methyl]indane hydr°Chloride benzaldehyde2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindane hydr°Chloride

4-[(2,3-二氢-5,6-二甲氧基-1H-茚-2-基)甲基]哌啶盐酸盐,苯甲醛置于sodium Cyanoborohydride体系中,用 甲醇,溶剂黄146 作为反应溶剂,化学反应 16.0H,以53%的收率获得产物多奈哌齐杂质d
参考文献:Novel Donepezil-Based Inhibitors Of Acetyl-And Butyrylcholinesterase And Acetylcholinesterase-Induced β-Amyloid Aggregation
标题:Novel Donepezil-Based Inhibitors Of Acetyl-And Butyrylcholinesterase And Acetylcholinesterase-Induced β-Amyloid Aggregation
摘要:A Novel Series Of Donepezil-Tacrine Hybrids Designed To Simultaneously Interact With The Active,Peripheral And Midgorge Binding Sites Of Acetylcholinesterase (Ache) Have Been Synthesized And Tested For Their Ability To Inhibit Ache,Butyrylcholinesterase (Bche),And Ache-Induced A Beta Aggregation. These Compounds Consist Of A Unit Of Tacrine Or 6-Chlorotacrine,Which occupies The Same Position As Tacrine At The Ache Active Site,And The 5,6-Dimethoxy-2-[(4-Piperidinyl)Methyl]-1-Indanone Moiety Of Donepezil (Or The Indane Derivative Thereof),Whose Position Along The Enzyme Gorge And The Peripheral Site Can Be Modulated By A Suitable Tether That Connects Tacrine And Donepezil Fragments. All Of The New Compounds Are Highly Potent Inhibitors Of Bovine And Human Ache And Bche,Exhibiting Ic50 Values In The Subnanomolar Or Low Nanomolar Range In Most Cases. Moreover,Six Out Of The Eight Hybrids Of The Series,Particularly Those Bearing An Indane Moiety,Exhibit A Significant A Beta Antiaggregating Activity,Which Makes Them Promising Anti-Alzheimer Drug Candidates.
DOI:10.1021/jm8001313

专利信息

专利号:US-2009298879-A1
优先权日:2006-05-18
标 题 :Impurities of Donepezil
发明人：KRIZMANIC IRENA; LERMAN LIDIJA; SAMARDZIC ZRINKA; KACZOROWSKA KATARZYNA; MANIKOWSKI ANDRZEJ; ZIORO BARBARA; GREBENAR IVICA; KORUZNJAK JASNA DOGAN
权利人:PLIVA HRVATSKA D O O
摘要:The present invention relates to impurities of donepezil, or a pharmaceutically acceptable salt thereof, which may be produced during synthesis and storage of donepezil, or a pharmaceutically-acceptable salt thereof, and to methods of identifying such impurities. The invention also relates to the use of these impurities in analytical techniques and to product that contain certain low levels of these impurities in particular the following impurities are disclosed: formula (I) and formula (II).