CAS: 864082-47-3; N-(6-Fluoro-1H-Indazol-5-yl)-2-Methyl-6-Oxo-4-(4-(Trifluoromethyl)Phenyl)-1,4,5,6-Tetrahydropyridine-3-Carboxamide

上下游产品

4-[4-(trifluoromethyl)phenyl]-2-methyl-6-oxo-1,4,5,6-tetrahydro-3-pyridinecarboxylic acid 5-amino-6-fluoro-1H-indazole methyl 4-[4-(trifluoromethyl)phenyl]-2-methyl-6-oxo-1,4,5,6-tetrahydro-3-pyridinecarboxylate 4-Trifluoromethylbenzaldehyde

Methyl 4-[4-(Trifluoromethyl)Phenyl]-2-Methyl-6-Oxo-1,4,5,6-Tetrahydro-3-Pyridinecarboxylate置于4-二甲氨基吡啶 Sodium Hydroxide,1-(3-二甲基氨基丙基)-3-乙基碳二亚胺,三乙胺体系中,用 甲醇,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 2.0H,反应生成 N-(6-氟-1H-吲唑-5-基)-2-甲基-6-氧代-4-[4-(三氟甲基)苯基]-1,4,5,6-四氢-3-吡啶甲酰胺
参考文献:Development Of Dihydropyridone Indazole Amides As Selective Rho-Kinase Inhibitors
标题:Development Of Dihydropyridone Indazole Amides As Selective Rho-Kinase Inhibitors
摘要:Rho Kinase (Rock1) Mediates Vascular Smooth Muscle Contraction And Is A Potential Target For The Treatment Of Hypertension And Related Disorders. Indazole Amide 3 Was Identified As A Potent And Selective Rock1 Inhibitor But Possessed Poor Oral Bioavailability. Optimization Of This Lead Resulted In The Discovery Of A Series Of Dihydropyridones,Exemplified By 13,With Improved Pharmacokinetic Parameters Relative To The Initial Lead. Indazole Substitution Played A Critical Role In Decreasing Clearance And Improving Oral Bioavailability.
DOI:10.1021/jm0609014