CAS: 158778-58-6; 3-((2'-(2H-Tetrazol-5-yl)-[1,1'-Biphenyl]-4-yl)Methyl)-2-Propyl-1,3-Diazaspiro[4.4]Non-1-En-4-One

该化合物是主要通过CYP2C9 介导氧化法形成的抗血压药物Irbesartan的一种活性代谢物,它展示了强力和选择性的II型血管抗体性1(AT1),有助于Irbesartan的治疗效应,该代谢物显示了母体的类似药理活动,其研究表明其在持续血压控制中的作用,其结构改变增强了AT1受体的结合性,改善了目标特性.Demetime Irbesartan由于在药物代谢作用和治疗监测的潜在影响,因此对药源性研究感兴趣.该代谢物的分析标准用于评估药物的处置和代谢途径.

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MSDS等安全信息

    上下游产品

    4'-(2-propyl-4-oxo-1,3-diaza-spiro[4.4]non-1-en-3-ylmethyl)biphenyl-2-carbonitrile 24H29N3O3C24H29N3O3 24H27N3O2C24H27N3O2 1-butyrylamino-cyclopentanecarboxylic acid (2'-cyano-biphenyl-4-ylmethyl)-amide

    合成工艺路线路线简述

      📜环亮氨酸置于sodium Hydroxide,Sodium Azide,三丁基氯化锡,1-羟基苯并三唑,N,N'-二环己基碳二亚胺,三氟乙酸体系中,用 二氯甲烷,邻二甲苯,水,甲苯 用作溶剂,化学反应 2.0H,反应生成去甲基厄贝沙坦
      参考文献:A New Entry To Antihypertensive Active Pharmaceutical Ingredient,Irbesartan And Its Analogues
      标题:A New Entry To Antihypertensive Active Pharmaceutical Ingredient,Irbesartan And Its Analogues
      摘要:
      Doi:10.1515/hc.2006.12.5.323

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      主要参考文献

      参考标题:A Novel Approach For The Conversion Of Primary Amides Into Tetrazoles By Using Tributyltin Chloride And Sodium Azide In The Presence Of Dmf
      作者:Ramesh Dandala,Korrapati Rao,Vijay Handa,Inti Rao,Ananta Rani,Sripelly Shivashankar,Andra Naidu
      摘要:A Novel And Efficient One-Pot Synthesis Of Tetrazole -Derivatives Such As Irbesartan And Its Analogues Has Been Described From The Primary Acid Amide Derivatives. Thus 2-Alkyl-3-[ P-( O-Amidophenyl)Benzyl]-1,3-Diazaspiro[4.4]Non-1-En-4-One Derivatives Or 4-[α-(Acylamino)Cyclopentamidomethyl]-2′-Carboxamidobi-Phenyl Derivatives Were Treated With Tributyltin Chloride And Sodium Azide In O-Xylene In The

      合成参考文献

      合成方法参考DOI号:10.1515/HC.2006.12.5.323
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