CAS: 1034439-57-0; Donepezil Impurity 5 (Hydrochloride)

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CAS号844694-84-4 1-benzyl-4-[(5,...

📜多奈哌齐杂质d置于盐酸体系中,用 甲醇,二氯甲烷 用作溶剂,以161 Mg的收率获得1-苄基-4-((5,6-二甲氧基-2,3-二氢-1H-茚-2-基)甲基)哌啶盐酸盐
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