(2S,3aS,7aS)-1-[(2S)-2-(3-环己基-2,4-二氧代-5-丙基-1-咪唑烷基)-1-氧代丙基]八氢-1H-吲哚-2-羧酸 | 353777-66-9

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: (2S,3aS,7aS)-1-[(2S)-2-(3-环己基-2,4-二氧代-5-丙基-1-咪唑烷基)-1-氧代丙基]八氢-1H-吲哚-2-羧酸
• 英文名称: (2S,3aS,7aS)-1-((2S)-2-((5RS)-3-Cyclohexyl-2,4-dioxo-5-propylimidazolidin-1-yl)propanoyl)octahydro-1H-indole-2-carboxylic acid
• 英文别名: (2S,3aS,7aS)-1-[(2S)-2-(3-cyclohexyl-2,4-dioxo-5-propylimidazolidin-1-yl)propanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carboxylic acid
• CAS: 353777-66-9
• 化学式: C₂₄H₃₇N₃O₅
• 分子量: 447.6
• InChiKey: LVXYHZNEZMQVIT-KYCCPTNOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  32
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  98.2
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• [EN] PROCESS FOR PURE PERINDOPRIL TERT-BUTYLAMINE SALT<br/>[FR] PROCEDE DE PRODUCTION DE SEL DE TERT-BUTYLAMINE DE PERINDOPRIL PUR
  申请人：HETERO DRUGS LTD

  公开号：WO2005019173A1

  公开（公告）日：2005-03-03

  Pure perindopril tert-butylamine salt is obtained by extracting an aqueous solution of perindopril or its salt contaminated with impurities with a suitable organic solvent such as methylenedichloride at a pH of 4.0 to 6.5, separating the organic layer, isolating perindopril from the organic layer and converting it into tert-butylamine salt.

  通过用适当的有机溶剂（如亚甲基二氯甲烷）提取受杂质污染的贝利多普利或其盐的水溶液，在pH值为4.0至6.5的条件下，得到纯的贝利多普利叔丁胺盐，分离有机层，从有机层中分离出贝利多普利并将其转化为叔丁胺盐。
• Process for manufacture of pure (2S, 3aS, 7aS)-1-[(2S)-2-[[(1S)-1-(ethoxycarbonyl) butyl] amino]-1-oxopropyl] octahydro-1H-indole-2-carboxylic acid and its tert. butyl amine salt
  申请人：Gunjal Tukaram Sanjay

  公开号：US20070021490A1

  公开（公告）日：2007-01-25

  New compounds useful as synthetic intermediates to synthesize perindopril, a new process for synthesizing perindopril, and new salts of perindopril.

  新化合物可用作合成前体，用于合成贝那普利，一种合成贝那普利的新工艺，以及贝那普利的新盐。
• Process for the preparation of high purity perindopril
  申请人：Simig Guyla

  公开号：US20070197821A1

  公开（公告）日：2007-08-23

  The invention relates to 1-2(S)-[1(S)-(ethoxycarbonyl)butylamino]propionyl}-(3aS,7aS)octahydroindol-2(S)-carboxylic acid of the Formula I and the t-butylamine salt of the Formula I′ thereof free of contaminations derivable from dicyclohexyl carbodiimide, and a process for the preparation thereof. The invention also relates to new intermediates of the general Formula III (wherein R stands for lower alkyl or aryl lower alkyl). The compound of the Formula I—perindopril—is a known ACE inhibitor.

  本发明涉及公式I的1-2(S)-[1(S)-(ethoxycarbonyl)butylamino]propionyl}-(3aS,7aS)八氢吲哚-2(S)-羧酸及其不含二环己基氨基甲酸酯污染物的t-丁基胺盐的制备方法。本发明还涉及一般公式III的新中间体（其中R代表低碳基或芳基低碳基）。公式I化合物perindopril是一种已知的ACE抑制剂。
• Process for the Purification of Perindopril
  申请人：Singh Girij Pal

  公开号：US20080139823A1

  公开（公告）日：2008-06-12

  A dicyclohexyamine salt of compound of formula I, namely perindopril, having an X-ray powder diffraction pattern with characteristic peaks (2θ): 8.462, 10.624, 18.693, 9.424, 17.272, 14.177, 19.499, 20.765, 21.409, and 14.540. A process for preparation of the said salt of perindopril and its use in the purification of an impure perindopril and a process for purification of perindropril comprising formation of its salt with dicyclohexylamine. The present invention also relates to preparation of Perindopril tert-butyl amine salt directly from Perindopril dicyclohexylamine salt without isolating the free base.
• PERINDOPRIL FORMULATIONS
  申请人：Subramony Janardhanan Anand

  公开号：US20100076052A1

  公开（公告）日：2010-03-25

  Pharmaceutical formulations comprising perindopril or its salts, isomers, enantiomers, polymorphs, metabolites, solvates, hydrates, and mixtures thereof, and at least one surface stabilizer. Also disclosed are methods of stabilizing perindopril in the formulations, and polyoxyethylene-polyoxypropylene block copolymers as surface stabilizers.