CAS: 445218-61-1; Topiroxostat Impurity 38

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4329-75-3 13025-99-5 54-92-2

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pyridine-4-carbonitrile isoniazid3,5-di(pyridin-4-yl)-1,2,4-triazole

📜4-氰基吡啶,异烟肼置于甲醇,Sodium Methylate体系中,用 甲醇 作为反应溶剂,化学反应 1.0H,反应生成 托匹司他杂质2
参考文献:Discovery Of 3-(3-Cyano-4-Pyridyl)-5-(4-Pyridyl)-1,2,4-Triazole,Fyx-051-A Xanthine Oxidoreductase Inhibitor For The Treatment Of Hyperuricemia
标题:Discovery Of 3-(3-Cyano-4-Pyridyl)-5-(4-Pyridyl)-1,2,4-Triazole,Fyx-051-A Xanthine Oxidoreductase Inhibitor For The Treatment Of Hyperuricemia
摘要:Our Previous Study Identified 2-[2-(2-Methoxy-Ethoxy)-Ethoxy]-5-[5-(2-Methyl-4-Pyridyl)-1H-[1,2,4]-Triazol-3-Yl]-Benzonitrile (2) As A Safe And Potent Xanthine Oxidoreductase (Xor) Inhibitor For The Treatment Of Hyperuricemia. Here,We Synthesized A Series Of 3,5-Dipyridyl-1,2,4-Triazole Derivatives And,In Particular,Examined Their In Vivo Activity In Lowering The Serum Uric Acid Levels In Rats. As A Result,We Identified 3-(3-Cyano-4-Pyridyl)-5-(4-Pyridyl)-1,2,4-Triazole (Fyx-051,Compound 39) To Be One Of The Most Potent Xor Inhibitors; It Exhibited An Extremely Potent In Vivo Activity,Weak Cyp3A4-Inhibitory Activity And A Better Pharmacokinetic Pro. Le Than Compound 2. Compound 39 Is Currently Being Evaluated In A Phase 2 Clinical Trial. (C) 2009 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmcl.2009.08.091