CAS: 286961-15-7; Benzyl 4-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)-5,6-Dihydropyridine-1(2H)-Carboxylate

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CAS号73183-34-3 双戊酰二硼 | CAS号286961-24-8 4-(三氟甲基磺酰氧基)-5,... | CAS号1121057-75-7 1,2,3,6-四氢-4-(4... | CAS号501-53-1 氯甲酸苄酯 | CAS号19099-93-5 1-Cbz-4-哌啶酮 | CAS号67259-62-5 4-(4-甲氧基苯基)哌啶 | CAS号1251537-33-3 (1-((苄氧基)羰基)-1,... | CAS号630116-81-3 2-(4-哌啶基)烟腈

1-Cbz-4-哌啶酮置于1,1'-双(二苯基膦)二茂铁,(1,1'-Bis(Diphenylphosphino)Ferrocene)Palladium(II) Dichloride,Potassium Acetate,Lithium Hexamethyldisilazane体系中,用 四氢呋喃,1,4-二氧六环 用作溶剂,化学反应 20.0H,反应生成N-苄氧羰基-3,6-二氢-2H-吡啶-4-硼酸频哪醇酯
参考文献:Discovery Of 3-Methyl-N-(1-Oxy-3',4',5',6'-Tetrahydro-2'h-[2,4'-Bipyridine]-1'-Ylmethyl)Benzamide (Abt-670),An Orally Bioavailable Dopamine D4 Agonist For The Treatment Of Erectile Dysfunction
标题:Discovery Of 3-Methyl-N-(1-Oxy-3',4',5',6'-Tetrahydro-2'h-[2,4'-Bipyridine]-1'-Ylmethyl)Benzamide (Abt-670),An Orally Bioavailable Dopamine D4 Agonist For The Treatment Of Erectile Dysfunction
摘要:The Goal Of This Study Was To Identify A Structurally Distinct D-4-Selective Agonist With Superior Oral Bioavailability To Our First-Generation Clinical Candidate 1A (Abt-724) For The Potential Treatment Of Erectile Dysfunction. Arylpiperazines Such As (Heteroarylmethyl) Piperazine 1A,Benzamide 2,And Acetamides Such As 3A,B Exhibit Poor Oral Bioavailability. Structure-Activity Relationship (Sar) Studies With The Arylpiperidine Template Provided Potent Partial Agonists Such As 4D And 5K That Demonstrated No Improvement In Oral Bioavailability. Further Optimization With The (N-Oxy-2-Pyridinyl) Piperidine Template Led To The Discovery Of Compound 6B (Abt-670),Which Exhibited Excellent Oral Bioavailability In Rat,Dog,And Monkey (68%,85%,And 91%,Respectively) With Comparable Efficacy,Safety,And Tolerability To 1A. The N-Oxy-2-Pyridinyl Moiety Not Only Provided The Structural Motif Required For Agonist Function But Also Reduced Metabolism Rates. The Sar Study Leading To The Discovery Of 6B Is Described Herein.
Doi:10.1021/jm060662K