3-O-ethyl 5-O-methyl (4S)-2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate;methanesulfonic acid | 401511-24-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 3-O-ethyl 5-O-methyl (4S)-2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate;methanesulfonic acid
• CAS: 401511-24-8
• 化学式: C21H29ClN2O8S
• 分子量: 505.0
• InChiKey: MUVFCHUBATVFPP-LMOVPXPDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.77
• 重原子数：
  33
• 可旋转键数：
  10
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  163
• 氢给体数：
  3
• 氢受体数：
  10

文献信息

• Process for making amlodipine, derivatives therof, and precursors therefor
  申请人：——

  公开号：US20020143046A1

  公开（公告）日：2002-10-03

  Amlodipine and related analogues thereof are prepared by the following general reaction scheme: 1 R 1 and R 2 each independently represent a C 1 -C 4 alkyl group. The process provides for the formation of compounds of formula (1) in good yield and purity. Further, the compounds of formula (1) can be used as calcium channel blockers or as reference standards or reference markers for checking the purity of amlodipine.

  氨氯地平及其相关类似物是通过以下一般反应方案制备的：1R1和R2各自独立表示C1-C4烷基基团。该过程提供了以良好产率和纯度形成化合物的方法。此外，化合物的公式（1）可用作钙通道阻滞剂，或用作氨氯地平纯度检查的参考标准或参考标记。
• [EN] ISOLATION OF DIHYDROPYRIDINE DERIVATIVE AND PREPARATION SALTS THEREOF<br/>[FR] ISOLATION DE DERIVE DE DIHYDROPYRIDINE ET SELS DE PREPARATION DE CELUI-CI
  申请人：EOS ECZACIBASI OZGUN KIMYASAL

  公开号：WO2004058711A1

  公开（公告）日：2004-07-15

  The title compound is isolated in pure form by using a crystallization process and converted to its pharmaceutically acceptable salts. The crystallization process affects stability and purity of the amlodipine salts. All known impurities and one unknown impurity, which forms during the synthesis of the amlodipine salts, were isolated, characterized, and synthesized. A new method allowing the quantitative HPLC analysis of all related impurities of amlodipine salts in a single chromatogram was developed.

  该化合物的标题化合物通过结晶过程纯化并转化为其药用可接受的盐。结晶过程影响氨氯地平盐的稳定性和纯度。所有已知杂质和在氨氯地平盐合成过程中形成的一种未知杂质均被分离、表征和合成。开发了一种新方法，允许在单个色谱图中定量HPLC分析氨氯地平盐的所有相关杂质。
• [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。
• Process for making amlodipine maleate
  申请人：——

  公开号：US20020086888A1

  公开（公告）日：2002-07-04

  A process for making amlodipine maleate comprises reacting amlodipine or an acid addition salt thereof with maleic acid under an acidic environment to form an amlodipine maleate product. The process allows for the formation of amlodipine maleate substantially free from amlodipine aspartate.

  制备氨氯地平马来酸盐的过程包括在酸性环境下将氨氯地平或其酸加成盐与马来酸反应，形成氨氯地平马来酸盐产品。该过程允许形成基本不含有氨氯地平天冬氨酸盐的氨氯地平马来酸盐。
• CETP inhibitors in combination with antihypertensive agents and uses thereof
  申请人：Pfizer Inc.

  公开号：US20040039018A1

  公开（公告）日：2004-02-26

  This invention relates to pharmaceutical combinations of a cholesteryl ester transfer protein (CETP) inhibitor or a pharmaceutically acceptable salt thereof; and an antihypertensive agent or a pharmaceutically acceptable salt thereof, optionally in combination with an HMG CoA reductase inhibitor or a pharmaceutically acceptable salt thereof, kits containing such combinations and methods of using such combinations to treat subjects suffering from atherosclerosis, peripheral vascular disease, dyslipidemia, hyperbetaliproteinemia, hypoalphalipoproteinemia, hypercholesterolemia, hypertriglyceridemia, familial-hypercholesterolemia, cardiovascular disorders, angina, ischemia, cardiac ischemia, stroke, myocardial infarction, reperfusion injury, angioplastic restenosis, hypertension, vascular complications of diabetes, obesity or endotoxemia in a mammal (including a human being either male or female).

  本发明涉及一种胆固醇酯转移蛋白（CETP）抑制剂或其药学上可接受的盐与降压药剂或其药学上可接受的盐的药物组合，可选地与HMG CoA还原酶抑制剂或其药学上可接受的盐的药物组合，包含这种组合的套件以及使用这种组合治疗患有动脉粥样硬化、外周血管疾病、血脂异常、高β脂蛋白血症、低α脂蛋白血症、高胆固醇血症、高三酰甘油血症、家族性高胆固醇血症、心血管疾病、心绞痛、缺血、心肌缺血、中风、心肌梗死、再灌注损伤、血管成形术再狭窄、高血压、糖尿病血管并发症、肥胖或内毒素血症的哺乳动物（包括男性或女性人类）的使用方法。