droxidopa hydrochloride | 1260173-94-1

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: droxidopa hydrochloride
• 英文别名: Droxidopa (hydrochloride)；(2S,3R)-2-amino-3-(3,4-dihydroxyphenyl)-3-hydroxypropanoic acid;hydrochloride
• CAS: 1260173-94-1
• 化学式: C₉H₁₁NO₅*ClH
• 分子量: 249.651
• InChiKey: FFEWFMCABUNGJJ-KZYPOYLOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.04
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  124
• 氢给体数：
  6
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  droxidopa hydrochloride 在 三乙胺 作用下， 以 甲醇 、 水 为溶剂， 以76.5%的产率得到屈西多巴
  参考文献：
  名称：

  [EN] AN IMPROVED PROCESS FOR THE PREPARATION OF DROXIDOPA AND ITS INTERMEDIATE
  [FR] PROCÉDÉ AMÉLIORÉ DE PRÉPARATION DE DROXIDOPA ET SON INTERMÉDIAIRE

  摘要：

  The present invention provides an improved process for preparation of the L-threo-(2S,3R)-3-(3,4-dihydroxyphenyl)serine (I) or a salt thereof, which is known as Droxidopa; comprising (a) recovery of the by-product compound (V) (as described herein) from the crude compound (I), and (b) recycling and re-use it for the preparation of droxidopa. Accordingly, the present invention relates to an improved economical process for the preparation of L-threo-(2S,3R)-3-(3.4-dihydroxyphenyl)serine (I) or its pharmaceutically acceptable salts; wherein the process relates to recovery and recycling of the by-product compound (V) and also to re-use it for the preparation of droxidopa.

  公开号：

  WO2019135189A1
• 作为产物：
  描述：

  在 盐酸 、 水 作用下， 以 甲醇 为溶剂， 反应 3.0h， 以40 g的产率得到droxidopa hydrochloride
  参考文献：
  名称：

  [EN] AN IMPROVED PROCESS FOR THE PREPARATION OF DROXIDOPA AND ITS INTERMEDIATE
  [FR] PROCÉDÉ AMÉLIORÉ DE PRÉPARATION DE DROXIDOPA ET SON INTERMÉDIAIRE

  摘要：

  The present invention provides an improved process for preparation of the L-threo-(2S,3R)-3-(3,4-dihydroxyphenyl)serine (I) or a salt thereof, which is known as Droxidopa; comprising (a) recovery of the by-product compound (V) (as described herein) from the crude compound (I), and (b) recycling and re-use it for the preparation of droxidopa. Accordingly, the present invention relates to an improved economical process for the preparation of L-threo-(2S,3R)-3-(3.4-dihydroxyphenyl)serine (I) or its pharmaceutically acceptable salts; wherein the process relates to recovery and recycling of the by-product compound (V) and also to re-use it for the preparation of droxidopa.

  公开号：

  WO2019135189A1

文献信息

• Process for the preparation of droxidopa and its intermediate
  申请人：PIRAMAL PHARMA LIMITED

  公开号：US11192848B2

  公开（公告）日：2021-12-07

  The present invention provides an improved process for preparation of the L-threo-(2S,3R)-3-(3 4-dihydroxyphenyl)serine (I) or a salt thereof, which is known as Droxidopa; comprising (a) recovery of the by-product compound (V) (as described herein) from the crude compound (I), and (b) recycling and re-use it for the preparation of droxidopa. Accordingly, the present invention relates to an improved economical process for the preparation of L-threo-(2S,3R)-3-(3.4-dihydroxyphenyl)serine (I) or its pharmaceutically acceptable salts; wherein the process relates to recovery and recycling of the by-product compound (V) and also to re-use it for the preparation of droxidopa.

  本发明提供了一种制备 L-硫代-(2S,3R)-3-(3.4-二羟基苯基)丝氨酸(I)或其盐(称为屈昔多巴)的改进工艺，包括(a)从粗化合物(I)中回收副产物化合物(V)(如本文所述)，以及(b)回收并再次用于制备屈昔多巴。因此，本发明涉及一种制备 L-苏-(2S,3R)-3-(3.4-二羟基苯基)丝氨酸(I)或其药学上可接受的盐的改进的经济工艺；其中该工艺涉及副产物化合物(V)的回收和循环利用，还涉及将其重新用于制备屈昔多巴。
• AN IMPROVED PROCESS FOR THE PREPARATION OF DROXIDOPA AND ITS INTERMEDIATE
  申请人：Piramal Enterprises Limited

  公开号：EP3436426A1

  公开（公告）日：2019-02-06