(1R,2S)-2-(3,4-difluorophenyl)-2-methylcyclopropan-1-amine

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (1R,2S)-2-(3,4-difluorophenyl)-2-methylcyclopropan-1-amine
• 化学式: C₁₀H₁₁F₂N
• 分子量: 183.2
• InChiKey: CYEXEDSBRZSYHU-ZJUUUORDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• NOVEL PROCESSES FOR THE PREPARATION OF PHENYLCYCLOPROPYLAMINE DERIVATIVES AND USE THEREOF FOR PREPARING TICAGRELOR
  申请人：Actavis Group PTC ehf

  公开号：US20140350301A1

  公开（公告）日：2014-11-27

  Provided herein are novel processes for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein are novel, commercially viable and industrially advantageous processes for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. Provided further herein are novel acid addition salts of trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine, and process for their preparation. The intermediate and its acid addition salts are useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity.

  本文提供了一种制备苯基环丙胺衍生物的新工艺，这些衍生物是制备嘧啶并三唑[4,5-d]化合物的有用中间体。本文特别提供了一种新的商业可行和工业优越的工艺，用于制备高纯度的替卡格雷尔中间体，即反式-(1R,2S)-2-(3,4-二氟苯基)-环丙胺。本文还提供了反式-(1R,2S)-2-(3,4-二氟苯基)-环丙胺的新酸加成盐及其制备工艺。该中间体及其酸加成盐可用于高产率和纯度制备替卡格雷尔或其药物可接受盐。