CAS: 63843-83-4; 1-Benzyl-4-Phenylpiperidin-4-Ol

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CAS号108-86-1 溴苯 | CAS号3612-20-2 N-苄基-4-哌啶酮 | CAS号591-51-5 苯基锂 | CAS号591-50-4 碘苯 | CAS号100-59-4 苯基氯化镁 | CAS号40807-61-2 4-羟基-4-苯基哌啶 | CAS号100-39-0 溴化苄 | CAS号100-44-7 氯化苄 | CAS号43064-12-6 4-苯基-1,2,3,6-四氢吡啶盐酸盐 | CAS号40807-61-2 4-羟基-4-苯基哌啶 | CAS号146396-04-5 4-(乙酰氨基)-4-苯基哌啶 | CAS号182621-56-3 N-甲基-4-苯基-4-哌啶胺 | CAS号771-99-3 4-苯基哌啶 | CAS号10272-49-8 4-苯基哌啶盐酸盐 | CAS号34273-01-3 4-N-甲基苄基-n-乙氧甲酰... | CAS号172733-78-7 4-(乙酰氨基)-1-苄基-4-苯基哌啶 | CAS号182621-52-9 4-(乙酰基氨基)-4-苯基-... | CAS号182621-53-0 4-[乙酰基(甲基)氨基]-4...

📜4-哌啶酮置于potassium Carbonate,Magnesium体系中,用 四氢呋喃,乙腈 作为反应溶剂,化学反应 20.17H,反应生成 1-苄基-4-苯基哌啶-4-醇
参考文献:Structure-Guided Design And Synthesis Of P1' Position 1-Phenylcycloalkylamine-Derived Pentapeptidic Bace1 Inhibitors
标题:Structure-Guided Design And Synthesis Of P1' Position 1-Phenylcycloalkylamine-Derived Pentapeptidic Bace1 Inhibitors
摘要:Previously,We Reported Potent Pentapeptidic Bace1 Inhibitors With The Hydroxymethylcarbonyl Isostere As A Substrate Transition-State Mimic. To Improve The In Vitro Potency,We Further Reported Pentapeptidic Inhibitors With Carboxylic Acid Bioisosteres At The P-4 And P-1' Positions. In The Current Study,We Screened New P-1' Position 1-Phenylcycloalkylamine Analogs To Find Non-Acidic Inhibitors That Possess Double-Digit Nanomolar Range Ic50 Values. An Extensive Structure-Activity Relationship Study Was Performed With Various Amine Derivatives At The P-1' Position. The Most Potent Inhibitor Of This Pentapeptide Series,Kmi-1830,Possessing 1-Phenylcyclopentylamine At The P-1' Position Had An Ic50 Value Of 11.6 Nm Against Bace1 In Vitro Enzymatic Assay. (C) 2011 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmc.2011.07.002

专利信息

专利号:RU-2143425-C1
优先权日:1994-03-18
标 题:Derivatives of piperidine, their salts, methods of their synthesis, pharmaceutical composition based on thereof and intermediate substances