amlodipine besylate dihydrate | 532929-68-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: amlodipine besylate dihydrate
• 英文别名: Amlodipine besylate monohydrate；benzenesulfonic acid;3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate;hydrate
• CAS: 532929-68-3；532929-67-2
• 化学式: C₆H₆O₃S*C₂₀H₂₅ClN₂O₅*2H₂O
• 分子量: 603.09
• InChiKey: HCCDDRGYEWJVFQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.37
• 重原子数：
  39
• 可旋转键数：
  11
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  164
• 氢给体数：
  4
• 氢受体数：
  11

文献信息

• [EN] TWO CRYSTALLINE HYDRATE FORMS OF AMLODIPINE BENZENESULFONATE OF HIGH PURITY, PROCESSES FOR THEIR PREPARATION AND USE<br/>[FR] DEUX FORMES DIHYDRATE CRISTALLIN DE BENZENESULFONATE D'AMLODIPINE A PURETE ELEVEE, LEURS PROCEDES DE PREPARATION ET LEUR UTILISATION
  申请人：LEK PHARMACEUTICALS

  公开号：WO2003101965A1

  公开（公告）日：2003-12-11

  The novel crystalline amlodipine benzenesulfonate dihydrate of high purity is disclosed, as well as the process for preparation of the novel crystalline amlodipine benzenesulfonate dihydrate of high purity and the crystalline amlodipine benzenesulfonate monohydrate of high purity, suitable for the preparation of pharmaceutical formulations for the treatment of cardiac diseases or hypertension, and their use as intermediate compounds in the improved process of purification of the nonhydrate benzenesulfonate (besylate) salt of amlodipine.The process for preparation of the crystalline amlodipine benzenesulfonate dihydrate is carried in the way that from the C1-C5 alcoholic solution of amlodipine benzenesulfonate with water while stirring at a temperature of 20°C or lower the crystals of pure amlodipine benzenesulfonate dihydrate are separated, and isolated.The process for preparation of the crystalline amlodipine benzenesulfonate monohydrate is carried in the way that from the C1-C5 alcoholic solution of amlodipine benzenesulfonate with water while stirring at a temperature of 30°C or higher the crystals of pure amlodipine benzenesulfonate monohydrate are separated, and isolated.

  揭示了高纯度的新型结晶氨氯地平苯磺酸苄水合物，以及制备高纯度的新型结晶氨氯地平苯磺酸苄水合物和高纯度的结晶氨氯地平苯磺酸苄单水合物的过程，适用于制备用于治疗心脏疾病或高血压的药物配方，并将它们用作改进的非水合物苯磺酸苄酯盐（besylate）的氨氯地平纯化过程中的中间化合物。制备结晶氨氯地平苯磺酸苄水合物的过程是这样进行的：在20°C或更低温度下，从氨氯地平苯磺酸苄的C1-C5醇溶液中加入水搅拌，分离并提取出纯净的氨氯地平苯磺酸苄水合物晶体。制备结晶氨氯地平苯磺酸苄单水合物的过程是这样进行的：在30°C或更高温度下，从氨氯地平苯磺酸苄的C1-C5醇溶液中加入水搅拌，分离并提取出纯净的氨氯地平苯磺酸苄单水合物晶体。
• [EN] PROCESS FOR THE PREPARATION OF AMLODIPINE SALTS<br/>[FR] PROCEDE POUR L'ELABORATION DE SELS D'AMLODIPINE
  申请人：CIPLA LTD

  公开号：WO2005023769A1

  公开（公告）日：2005-03-17

  A process for the preparation of salts of amlodipine comprises subjecting a compound of formula (II) to a deprotection reaction and converting the amlodipine free base thus obtained to a salt (1) without isolating amlodipine free base. Preferably, the maleate, besylate, malate or fumarate salt is made.

  一种制备氨氯地平盐的方法包括将式（II）的化合物进行去保护反应，并将得到的氨氯地平游离碱转化为盐（1），而无需分离氨氯地平游离碱。最好制备马来酸盐、苯磺酸盐、苹果酸盐或富马酸盐。
• COMPOSITION CONTAINING LEGOAMODIPINE BESYLATE HYDRATE AND PREPARATION METHOD THEREFOR
  申请人：Shihuida Pharmaceuticals Group (Jilin) Ltd.

  公开号：EP4023221A1

  公开（公告）日：2022-07-06

  The present invention relates to a composition comprising levamlodipine besylate hydrate and its production, pharmaceutical preparations and use, especially the composition of (S)-2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydro-3,5-pyridinedicarboxylic acid-3-ethyl ester, 5-methyl ester benzenesulfonic acid hydrate and its production method and use. The composition of levamlodipine besylate crystallized in pure water and dried is easy for industrial production, has no organic solvent residue, good thermal stability and good dissolution amount in solid-form preparations.

  本发明涉及一种由水合苯磺酸左旋氨氯地平组成的组合物及其生产、药物制剂和用途，特别是(S)-2-[(2-氨基乙氧基)甲基]-4-(2-氯苯基)-6-甲基-1,4-二氢-3,5-吡啶二羧酸-3-乙酯、5-甲酯苯磺酸水合物的组合物及其生产方法和用途。纯水干燥结晶的苯磺酸左旋氨氯地平组合物易于工业化生产，无有机溶剂残留，热稳定性好，在固体制剂中溶解度高。
• Amlodipine salt forms and processes for preparing them
  申请人：——

  公开号：US20030139455A1

  公开（公告）日：2003-07-24

  Amlodipine besylate forms are described, including amlodipine besylate hydrates and novel amlodipine besylate anhydrates. A method of making various amlodipine besylate forms from an aqueous medium as well as the use of the same as a calcium channel blocker are described.

  描述了苯磺酸氨氯地平的各种形式，包括苯磺酸氨氯地平水合物和新型苯磺酸氨氯地平无水物。还介绍了一种从水介质中制取各种苯磺酸氨氯地平的方法，以及将其用作钙通道阻滞剂的方法。
• AMLODIPINE SALT FORMS AND PROCESSES FOR PREPARING THEM
  申请人：Synthon B.V.

  公开号：EP1448197A1

  公开（公告）日：2004-08-25