tert-butyl N-((3S)-1-((3-hydroxyphenyl)methyl)pyrrolidin-3-yl)carbamate | 1246299-55-7

• 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: tert-butyl N-((3S)-1-((3-hydroxyphenyl)methyl)pyrrolidin-3-yl)carbamate
• 英文别名: (S)-tert-Butyl (1-(3-hydroxybenzyl)pyrrolidin-3-yl)carbamate；tert-butyl N-[(3S)-1-[(3-hydroxyphenyl)methyl]pyrrolidin-3-yl]carbamate
• CAS: 1246299-55-7
• 化学式: C₁₆H₂₄N₂O₃
• 分子量: 292.378
• InChiKey: JNVUTZKLLQDPIG-ZDUSSCGKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  21
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  61.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  tert-butyl N-((3S)-1-((3-hydroxyphenyl)methyl)pyrrolidin-3-yl)carbamate 在 盐酸 作用下， 以 1,4-二氧六环 为溶剂， 反应 2.0h， 以100%的产率得到3-{[(3S)-3-aminopyrrolidin-1-yl]methyl}phenol hydrochloride
  参考文献：
  名称：

  [EN] TOPICAL PHARMACEUTICAL COMPOSITIONS COMPRISING IMIDAZO[1,2-B]PYRIDAZINE COMPOUNDS
  [FR] COMPOSITIONS PHARMACEUTIQUES TOPIQUES COMPRENANT DES COMPOSÉS IMIDAZO[1,2-B]PYRIDAZINE

  摘要：

  本发明涉及药物组合物，例如局部药物组合物，包括某些咪唑[1,2-b]吡啶嗪化合物及该类化合物的药用可接受的盐和/或溶剂化合物。该发明还涉及制备药物组合物的方法，以及利用这些组合物治疗与肌浆蛋白相关激酶（Trk）活性相关的疾病或症状。更具体地，该发明涉及包含化合物（I）的局部药物组合物或其药用可接受的盐和/或溶剂化合物，这些组合物在抑制Trk方面是有用的。

  公开号：

  WO2021148805A1
• 作为产物：
  描述：

  间羟基苯甲醛 、 (S)-3-叔丁氧羰基氨基吡咯烷 在 溶剂黄146 、 三乙酰氧基硼氢化钠 作用下， 以 二氯甲烷 为溶剂， 反应 5.0h， 以100%的产率得到tert-butyl N-((3S)-1-((3-hydroxyphenyl)methyl)pyrrolidin-3-yl)carbamate
  参考文献：
  名称：

  [EN] TOPICAL PHARMACEUTICAL COMPOSITIONS COMPRISING IMIDAZO[1,2-B]PYRIDAZINE COMPOUNDS
  [FR] COMPOSITIONS PHARMACEUTIQUES TOPIQUES COMPRENANT DES COMPOSÉS IMIDAZO[1,2-B]PYRIDAZINE

  摘要：

  本发明涉及药物组合物，例如局部药物组合物，包括某些咪唑[1,2-b]吡啶嗪化合物及该类化合物的药用可接受的盐和/或溶剂化合物。该发明还涉及制备药物组合物的方法，以及利用这些组合物治疗与肌浆蛋白相关激酶（Trk）活性相关的疾病或症状。更具体地，该发明涉及包含化合物（I）的局部药物组合物或其药用可接受的盐和/或溶剂化合物，这些组合物在抑制Trk方面是有用的。

  公开号：

  WO2021148805A1

文献信息

• [EN] IMIDAZO[1,2-B]PYRIDAZINES AS TRK INHIBITORS<br/>[FR] IMIDAZO[1,2-B]PYRIDAZINES UTILISÉES EN TANT QU'INHIBITEURS DE TRK
  申请人：BENEVOLENTAI BIO LTD

  公开号：WO2020039209A1

  公开（公告）日：2020-02-27

  The present invention relates to certain imidazo[1,2-b]pyridazine compounds and the pharmaceutically acceptable salts of such compounds. The invention also relates to the processes for the preparation of the compounds, compositions containing the compounds, and the uses of such compounds and salts in treating diseases or conditions associated with tropomyosin-related kinase (Trk), activity. More specifically the invention relates to the compounds and their salts useful as inhibitors of Trk. Formula (I) wherein R1, R2, R3, R4 and R5, L and Z are as defined herein.

  本发明涉及某些咪唑并[1,2-b]吡啶嗪化合物以及这些化合物的药用盐。本发明还涉及制备这些化合物的过程、含有这些化合物的组合物、以及这些化合物和盐在治疗与肌浆蛋白相关激酶（Trk）活性相关的疾病或症状中的用途。更具体地，本发明涉及作为Trk抑制剂有用的化合物及其盐。公式（I）中R1、R2、R3、R4和R5、L和Z的定义如本文所述。
• IMIDAZO[1,2-B]PYRIDAZINES AS TRK INHIBITORS
  申请人：BenevolentAl Bio Limited

  公开号：US20210253572A1

  公开（公告）日：2021-08-19

  The present invention relates to certain imidazo[1,2-b]pyridazine compounds and the pharmaceutically acceptable salts of such compounds. The invention also relates to the processes for the preparation of the compounds, compositions containing the compounds, and the uses of such compounds and salts in treating diseases or conditions associated with tropomyosin-related kinase (Trk), activity. More specifically the invention relates to the compounds and their salts useful as inhibitors of Trk. Formula (I) wherein R 1 , R 2 , R 3 , R 4 and R 5 , L and Z are as defined herein.
• Chiral 3-aminopyrrolidines as a rigid diamino scaffold for organocatalysis and organometallic chemistry
  作者：Mickael Pouliquen、Jérôme Blanchet、Michaël De Paolis、B. Rema Devi、Jacques Rouden、Marie-Claire Lasne、Jacques Maddaluno

  DOI：10.1016/j.tetasy.2010.04.038

  日期：2010.6

  Over 20 new and easily prepared diamines were screened for the asymmetric Morita-Baylis-Hillman reaction. Chiral non-racemic 3-(N,N-dimethylamino)-1-methylpyrrolidine was found to promote efficiently the reaction of methyl vinyl ketone and substituted benzaldehydes. Enantiomeric excesses up to 73% were reached with electron-deficient benzaldehyde derivatives. After a simple deprotonation, one of these diamines was transformed into a chiral mixed aggregate for the enantioselective synthesis of (R)-1-o-tolylethanol with 76% ee. (C) 2010 Elsevier Ltd. All rights reserved.
• [EN] TOPICAL PHARMACEUTICAL COMPOSITIONS COMPRISING IMIDAZO[1,2-B]PYRIDAZINE COMPOUNDS<br/>[FR] COMPOSITIONS PHARMACEUTIQUES TOPIQUES COMPRENANT DES COMPOSÉS IMIDAZO[1,2-B]PYRIDAZINE
  申请人：BENEVOLENTAI BIO LTD

  公开号：WO2021148805A1

  公开（公告）日：2021-07-29

  The present invention relates to pharmaceutical compositions, such as topical pharmaceutical compositions, comprising certain imidazo[1,2-b]pyridazine compounds and the pharmaceutically acceptable salts and/or solvates of such compounds. The invention also relates to the processes for the preparation of the pharmaceutical compositions, and the uses of such compositions in treating diseases or conditions associated with tropomyosin-related kinase (Trk) activity. More specifically the invention relates to topical pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salts and/or solvates thereof, which are useful in inhibiting Trk.

  本发明涉及药物组合物，例如局部药物组合物，包括某些咪唑[1,2-b]吡啶嗪化合物及该类化合物的药用可接受的盐和/或溶剂化合物。该发明还涉及制备药物组合物的方法，以及利用这些组合物治疗与肌浆蛋白相关激酶（Trk）活性相关的疾病或症状。更具体地，该发明涉及包含化合物（I）的局部药物组合物或其药用可接受的盐和/或溶剂化合物，这些组合物在抑制Trk方面是有用的。