化合物 T0231L2 | 440358-84-9

• 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
• 中文名称: 化合物 T0231L2
• 英文名称: Amlodipine mesylate monohydrate
• 英文别名: 3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate;methanesulfonic acid;hydrate
• CAS: 440358-84-9
• 化学式: C21H31ClN2O9S
• 分子量: 523.0
• InChiKey: LGWOIMCQWJLZIT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.95
• 重原子数：
  34
• 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：
  164
• 氢给体数：
  4
• 氢受体数：
  11

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。
• MANUFACTURING METHOD AND APPARATUS OF ULTRAFINE PARTICLES HAVING UNIFORM PARTICLE SIZE DISTRIBUTION
  申请人：Hwang Sung Joo

  公开号：US20110200678A1

  公开（公告）日：2011-08-18

  The present invention relates to a novel technology for forming fine particles with a size of 0.02˜3 microns from a solid that can be dissolved in a liquid solvent and is not decomposed by heat. The particle preparation technology according to the present invention may be applicable to the fields of food, cosmetics, biopolymer, polymer compositions, and pharmaceuticals.

  本发明涉及一种新型技术，用于从可溶于液体溶剂且不会被热分解的固体中形成粒径为0.02〜3微米的细小颗粒。本发明的颗粒制备技术可适用于食品、化妆品、生物聚合物、聚合物组合物和制药等领域。
• [EN] PROCESS FOR PREPARING ALMODIPINE MESYLATE MONOHYDRATE<br/>[FR] PROCEDE DE PREPARATION DE MESYLATE D'AMLODIPINE MONOHYDRATE
  申请人：CIPLA LTD

  公开号：WO2004096770A1

  公开（公告）日：2004-11-11

  Amlodipine mesylate monohydrate is prepared either from anhydrous amlodipine mesylate, or in the presence of a water immiscible solvent medium from amlodipine free base and methane sulphonic acid.

  Amlodipine mesylate monohydrate可以从无水氯苯甲醚酸氨氯地平或者在水不相溶的溶剂介质中从氨氯地平和甲烷磺酸制备。
• Process for determining the purity of amlodipine
  申请人：Bioorganics B.V.

  公开号：EP1577298A1

  公开（公告）日：2005-09-21

  The invention relates to a process, which comprises assaying amlodipine, a pharmaceutically acceptable salt thereof, or a composition containing the same for the presence of at least one of specific compounds 1(b)-1(f), to a process of testing the purity of phthalimidoamlodipine, which comprises assaying phthalimidoamlodipine, a pharmaceutically acceptable salt thereof, or a composition containing the same for the presence of at least one of the specific compounds 2b-2e, and to a process of producing amlodipine, which comprises the steps of: (a) assaying a sample from a batch of phthalimidoamlodipine for at least one phthalimidoamlodipine impurity selected from the group consisting of the compounds 2b-2e: (b) determining whether said at least one phthalimidoamlodipine impurity is contained in said sample below a predetermined limit, and, if below said predetermined limit; (c) subjecting said phthalimidoamlodipine batch to deprotection to form a batch of amlodipine.

  本发明涉及一种方法，其包括检测氨氯地平、其药学上可接受的盐或含有其的组合物中是否存在特定化合物1(b)-1(f)中的至少一种，以及一种测试邻苯二甲酰亚氨基氨氯地平纯度的方法，其包括检测邻苯二甲酰亚氨基氨氯地平、其药学上可接受的盐或含有其的组合物中是否存在特定化合物2b-2e中的至少一种，并且涉及一种生产氨氯地平的方法，其包括以下步骤：(a)检测邻苯二甲酰亚氨基氨氯地平批次中的样品，至少包括化合物2b-2e中的一种邻苯二甲酰亚氨基氨氯地平杂质；(b)确定该至少一种邻苯二甲酰亚氨基氨氯地平杂质是否在预定限制以下，如果在预定限制以下；(c)对邻苯二甲酰亚氨基氨氯地平批次进行去保护作用，形成氨氯地平批次。