酒石酸阿福莫特罗杂质1 | 245759-62-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 酒石酸阿福莫特罗杂质1
• 英文名称: (R,R)-3-amino-α[[[2-(4-methoxyphenyl)-1-methylethyl](phenylmethyl)amino]methyl]-4-(phenylmethoxy)-benzenemethanol
• 英文别名: (alphaR)-3-Amino-4-hydroxy-alpha-[[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]methyl]benzenemethanol；2-amino-4-[(1R)-1-hydroxy-2-[[(2R)-1-(4-methoxyphenyl)propan-2-yl]amino]ethyl]phenol
• CAS: 245759-62-0
• 化学式: C₁₈H₂₄N₂O₃
• 分子量: 316.4
• InChiKey: AMISPUNGCBUARA-XIKOKIGWSA-N

物化性质

• 沸点：
  545.7±50.0 °C(Predicted)
• 密度：
  1.195±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  23
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  87.7
• 氢给体数：
  4
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  酒石酸阿福莫特罗杂质1 在 palladium 10% on activated carbon 氢气 作用下， 以 乙醇 、 乙二醇 为溶剂， 反应 5.0h， 生成 (R,R)-formoterol
  参考文献：
  名称：

  PURIFICATION PROCESS FOR PREPARING HIGHLY PURE ARFORMOTEROL TARTRATE SUBSTANTIALLY FREE OF DESFORMYL IMPURITY

  摘要：

  本文提供了一种高纯度的酒石酸阿福莫特罗尔或其无定形形式，基本上不含去甲酰杂质2-羟基-5-[(1R)-1-羟基-2-[[(1R)-2-(4-甲氧基苯基)-1-甲基乙基]氨基]乙基]苯胺，以及其制备方法和包含高纯度酒石酸阿福莫特罗尔、基本上不含去甲酰杂质的药物组合物。

  公开号：

  US20120053246A1

文献信息

• PROCESS FOR THE PREPARATION OF ARFORMOTEROL OR SALT THEREOF
  申请人：Glenmark Pharmaceuticals Limited

  公开号：US20160083334A1

  公开（公告）日：2016-03-24

  Provided is an improved process for the preparation of arformoterol L-(+)-tartrate, and more specifically provided is a novel process for the preparation of arformoterol L-(+)-tartrate via arformoterol D-(−)-tartrate.

  提供了一种改进的制备左旋侧流通气 L-(+)-酒石酸盐的方法，更具体地提供了一种通过左旋侧流通气 D-(−)-酒石酸盐制备左旋侧流通气 L-(+)-酒石酸盐的新方法。
• [EN] NEW POLYMORPHIC FORM OF A LONG-ACTING BETA-2 ADRENOCEPTOR AGONIST<br/>[FR] NOUVELLE FORME POLYMORPHE D'UN AGONISTE DU RÉCEPTEUR ADRÉNERGIQUE BÊTA-2 À ACTION PROLONGÉE
  申请人：LESVI LABORATORIOS SL

  公开号：WO2013136061A1

  公开（公告）日：2013-09-19

  New polymorphic form of a long-acting beta-2 adrenoceptor agonist A new polymorphic form of arformoterol tartrate, designated as form D, is provided and which is characterised by at least one of the following: (i) a powder X-ray diffraction pattern having peaks at approximately 6.8, 13.3, 13.6, 3.8, 14.1, 18.2, 18.7, 20.0 ±0.2 degrees two theta; or (ii) a DSC thermogram showing an endothermic peak with an onset at approximately 19-120 ºC, and a maximum at approximately 129-131 ºC, followed by an exothermic peak with a maximum at approximately 137-138 ºC; wherein the DSC thermogram of form D has a further endothermic peak with an onset at approximately 168-170 ºC.1 Processes for preparing the new polymorphic form, uses thereof and intermediates for the preparation thereof, are also provided.

  提供了一种新的β-2肾上腺素受体长效激动剂的多态形式，称为D型，其特征至少具有以下之一：（i）粉末X射线衍射图谱在约6.8、13.3、13.6、3.8、14.1、18.2、18.7、20.0±0.2度二θ处具有峰值；或（ii）DSC热重图谱显示一个起始于约19-120℃，最大值约为129-131℃的吸热峰，其后是一个最大值约为137-138℃的放热峰；其中，D型的DSC热重图谱具有进一步的起始于约168-170℃的吸热峰。还提供了制备新多态形式的方法、其用途以及制备中间体。
• POLYMORPHIC FORM OF A LONG-ACTING BETA-2 ADRENOCEPTOR AGONIST
  申请人：Laboratorios Lesvi S.L.

  公开号：US20150087715A1

  公开（公告）日：2015-03-26

  New polymorphic form of a long-acting beta-2 adrenoceptor agonist A new polymorphic form of arformoterol tartrate, designated as form D, is provided and which is characterised by at least one of the following: (i) a powder X-ray diffraction pattern having peaks at approximately 6.8, 13.3, 13.6, 3.8, 14.1, 18.2, 18.7, 20.0±0.2 degrees two theta; or (ii) a DSC thermogram showing an endothermic peak with an onset at approximately 19-120° C., and a maximum at approximately 129-131° C., followed by an exothermic peak with a maximum at approximately 137-138° C.; wherein the DSC thermogram of form D has a further endothermic peak with an onset at approximately 168-170° C.1 Processes for preparing the new polymorphic form, uses thereof and intermediates for the preparation thereof, are also provided.

  一种长效β-2肾上腺素受体激动剂的新多态形式 提供了一种新的arformoterol酒石酸盐的多态形式，称为D型，其特征至少包括以下一种：（i）粉末X射线衍射图谱在约6.8、13.3、13.6、3.8、14.1、18.2、18.7、20.0±0.2度的二θ处具有峰值；或（ii）DSC热重谱图显示一个在约19-120°C开始的内吸热峰，并在约129-131°C达到最大值，然后是一个在约137-138°C达到最大值的外放热峰；其中D型的DSC热重谱图具有进一步的内吸热峰，其开始于约168-170°C。还提供了制备新多态形式的工艺、其用途和制备中间体。
• Polymorphic form of a long-acting beta-2 adrenoceptor agonist
  申请人：Laboratorios Lesvi S.L.

  公开号：US09309186B2

  公开（公告）日：2016-04-12

  New polymorphic form of a long-acting beta-2 adrenoceptor agonist A new polymorphic form of arformoterol tartrate, designated as form D, is provided and which is characterized by at least one of the following: (i) a powder X-ray diffraction pattern having peaks at approximately 6.8, 13.3, 13.6, 3.8, 14.1, 18.2, 18.7, 20.0±0.2 degrees two theta; or (ii) a DSC thermogram showing an endothermic peak with an onset at approximately 19-120° C., and a maximum at approximately 129-131° C., followed by an exothermic peak with a maximum at approximately 137-138° C.; wherein the DSC thermogram of form D has a further endothermic peak with an onset at approximately 168-170° C.1 Processes for preparing the new polymorphic form, uses thereof and intermediates for the preparation thereof, are also provided.

  提供了一种新的长效β-2肾上腺素受体激动剂的多态形式——酒石酸阿福莫特罗的D型，其特征至少具有以下之一：（i）粉末X射线衍射图谱在大约6.8、13.3、13.6、3.8、14.1、18.2、18.7、20.0±0.2度2θ处具有峰值；或（ii）DSC热重谱图显示一个在大约19-120℃处开始，最大值在大约129-131℃处的吸热峰，接着是一个在大约137-138℃处最大值的放热峰；其中，D型的DSC热重谱图具有一个在大约168-170℃处开始的进一步的吸热峰。此外，还提供了制备新的多态形式的方法、其用途以及制备中间体。
• Formoterol tartrate process and polymorph
  申请人：Sepracor Inc.

  公开号：EP2165999A1

  公开（公告）日：2010-03-24

  A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.

  本发明公开了一种高纯度酒石酸 R,R-福莫特罗盐的制备方法。该方法通过重结晶一种新的多晶型态来提供热力学上最稳定的多晶型态。