(+/-) 1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethyl]amino-2-propanol salicylate | 787598-91-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: (+/-) 1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethyl]amino-2-propanol salicylate
• 英文别名: 1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol;2-hydroxybenzoic acid
• CAS: 787598-91-8
• 化学式: C₇H₆O₃*C₂₄H₂₆N₂O₄
• 分子量: 544.604
• InChiKey: OYDGTBUVLALRCK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.83
• 重原子数：
  40
• 可旋转键数：
  11
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  133
• 氢给体数：
  5
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  (+/-) 1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethyl]amino-2-propanol salicylate 在 sodium hydroxide 、 水 作用下， 以 异丙醇 为溶剂， 生成 卡维地洛
  参考文献：
  名称：

  WO2008/38301

  摘要：

  公开号：
• 作为产物：
  描述：

  2-甲氧基苯氧基乙胺 、 水杨酸 、 4-环氧丙烷氧基咔唑 以 异丙醇 为溶剂， 生成 (+/-) 1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethyl]amino-2-propanol salicylate
  参考文献：
  名称：

  WO2008/38301

  摘要：

  公开号：

文献信息

• [EN] PROCESS FOR THE PREPARATION OF CARVEDILOL FORM-II<br/>[FR] PROCEDE DE FABRICATION DE CARVEDILOL, FORME-II
  申请人：MATRIX LAB LTD

  公开号：WO2004094378A1

  公开（公告）日：2004-11-04

  The present invention provides a cost-effective, industrially feasible process for the manufacture of crystalline Carvedilol Form-II using novel Carvedilol salts comprising a step of reacting 4-(2,3-epoxy propoxy) carbazole (II) with 2-(2-methoxy phenoxy) ethyl amine (III) followed by acidification with mineral acid in presence of an organic solvent to yield acid addition salts, treatment of the said salts with base(s) in presence of organic solvent(s), water and isolation from the organic solvent(s) followed by crystallization from ethyl acetate.

  本发明提供了一种成本效益高、在工业上可行的过程，用于制备结晶的卡维地洛Ⅱ型，该过程使用包含与2-(2-甲氧基苯氧基)乙基胺(III)反应的4-(2,3-环氧丙氧基)咔唑(II)的新型卡维地洛盐，然后在有机溶剂存在下与矿酸反应酸化，得到酸加盐，用碱在有机溶剂和水的存在下处理所述盐，然后从有机溶剂中分离，最后从乙酸乙酯中结晶。
• Process For Manufacture of Racemic Carvedilol
  申请人：Shah Dhiraj R.

  公开号：US20080214833A1

  公开（公告）日：2008-09-04

  The invention relates to a novel process for the manufacture of Carvedilol of high HPLC purity (>99.5%) having individual impurity less than 0.1%. The product is isolated from reaction mass as a salt with suitable organic acids which on further purification is converted into the free base i.e., Carvedilol.

  本发明涉及一种新型的制备高HPLC纯度（>99.5%）的卡维地洛的工艺，其个别杂质小于0.1%。该产品从反应物中以适当的有机酸盐的形式分离出来，经过进一步的纯化后转化为游离基即卡维地洛。
• Process for the preparation of carvedilol form-ii
  申请人：Ramanjaneyulu Seeta Gorantla

  公开号：US20070055069A1

  公开（公告）日：2007-03-08

  The present invention provides a cost-effective, industrially feasible process for the manufacture of crystalline Carvedilol Form-II using novel Carvedilol salts comprising a step of reacting 4-(2,3-epoxy propoxy)carbazole (II) with 2-(2-methoxy phenoxy)ethyl amine (III) followed by acidification with mineral acid in presence of an organic solvent to yield acid addition salts, treatment of the said salts with base(s) in presence of organic solvent(s), water and isolation from the organic solvent(s) followed by crystallization from ethyl acetate.

  本发明提供了一种成本效益高、工业上可行的制备晶体卡维地洛二型的方法，使用新型卡维地洛盐，包括以下步骤：将4-(2,3-环氧丙氧基)咔唑（II）与2-(2-甲氧基苯氧基)乙基胺（III）反应，在有机溶剂存在下加入矿酸使其酸化形成酸加成盐，将所述盐在有机溶剂存在下与碱反应，加入水并从有机溶剂中分离，随后从乙酸乙酯中结晶。
• PROCESS FOR THE PREPARATION OF CARVEDILOL FORM II
  申请人：RAMANJANEYULU GORANTLA SEETA

  公开号：US20090286991A1

  公开（公告）日：2009-11-19

  A cost-effective, industrially feasible process for the manufacture of crystalline Carvedilol Form-II using novel Carvedilol salts comprises the steps of reacting 4-(2,3-epoxy propoxy)carbazole (II) with 2-(2-methoxy phenoxy)ethyl amine (III) followed by acidification with mineral acid in presence of an organic solvent to yield acid addition salts, treatment of the said salts with base(s) in presence of organic solvent(s), water and isolation from the organic solvent(s) followed by crystallization from ethyl acetate.

  一种经济实惠、工业可行的制备晶体卡维地洛II型的过程，使用新型卡维地洛盐，包括以下步骤：将4-(2,3-环氧丙氧基)咔唑（II）与2-(2-甲氧基苯氧基)乙基胺（III）反应，然后在有机溶剂存在下用矿物酸酸化，得到酸加成盐，将所述盐在有机溶剂和水存在下用碱处理，从有机溶剂中分离出来，然后从乙酸乙酯中结晶。
• [EN] PROCESS FOR MANUFACTURE OF RACEMIC CARVEDILOL<br/>[FR] PROCEDE DE PREPARATION DE CARVEDILOL RACEMIQUE
  申请人：CADILA HEALTHCAR LTD

  公开号：WO2005080329A3

  公开（公告）日：2006-09-28