(R)-2-氨基-3-甲氧基丙-1-醇 | 148278-96-0

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: (R)-2-氨基-3-甲氧基丙-1-醇
• 英文名称: (2R)-2-amino-3-methoxypropan-1-ol
• 英文别名: (R)-2-amino-3-methoxy propan-1-ol；(R)-2-amino-3-methoxy-propan-1-ol；(R)-2-amino-3-methoxypropan-1-ol；(R)-O-methylserinol
• CAS: 148278-96-0
• 化学式: C₄H₁₁NO₂
• 分子量: 105.137
• InChiKey: KRWNDTAVKGMNDQ-SCSAIBSYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.5
• 重原子数：
  7
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  55.5
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (R)-2-氨基-3-甲氧基丙-1-醇 、 1-萘甲酰氯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 20.0h， 以93%的产率得到(R)-2-amino-3-methoxy-N-naphthoyl-propan-1-ol
  参考文献：
  名称：

  Asymmetric Addition to Chiral Aromatic and Unsaturated Oxazolines Using a Novel Chiral Auxiliary

  摘要：

  通过利用S-丝氨酸，成功合成了还原的甲氧基氨醇（12）的两种对映体。由这些辅助试剂制备的相应噁唑啉在与萘（22）和环己烯（27）的加成反应中显示出良好的性能。

  DOI：

  10.1055/s-1993-25842
• 作为产物：
  描述：

  (S)-4-methoxymethyl-2-phenyl-oxazoline 在 盐酸 作用下， 以 水 为溶剂， 生成 (R)-2-氨基-3-甲氧基丙-1-醇
  参考文献：
  名称：

  Concise synthesis of (+)-serinolamide A

  摘要：

  Serinolamide A, isolated from a species of marine cyanobacteria, exhibits a moderate agonist effect and selectivity for the CB1 cannabinoid receptor, which is unusual for marine natural products. Herein, we reported a highly efficient enantiospecific first total synthesis of (+)-serinolamide A from L-serine in nine steps with 30% overall yield. The synthesis method provides a facile, practicable, and economical approach for the preparation of other similar endocanabinoid lipids. (C) 2013 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2013.09.084

文献信息

• [EN] 2-HETEROARYL-3-OXO-2,3-DIHYDROPYRIDAZINE-4-CARBOXAMIDES FOR THE TREATMENT OF CANCER<br/>[FR] 2-HÉTÉROARYL-3-OXO-2,3-DIHYDROPYRIDAZINE-4-CARBOXAMIDES POUR LE TRAITEMENT DU CANCER
  申请人：BAYER AG

  公开号：WO2018146010A1

  公开（公告）日：2018-08-16

  The present invention covers 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compounds of general formula (I), in which X, R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.

  本发明涵盖了一般式(I)的2-杂环芳基-3-酮基-2,3-二氢吡啶嗪-4-羧酰胺化合物，其中X、R1、R2、R3、R4和R5如本文所定义，制备所述化合物的方法，用于制备所述化合物的有用中间体化合物，包含所述化合物的药物组合物和组合物，以及利用所述化合物制造用于治疗或预防疾病的药物组合物，特别是癌症或与异常AHR信号传导相关的疾病，或与失调免疫反应或其他与异常AHR信号传导相关的疾病，作为单一药剂或与其他活性成分组合使用。
• PYRIDAZINONES AS PARP7 INHIBITORS
  申请人：Ribon Therapeutics Inc.

  公开号：US20190330194A1

  公开（公告）日：2019-10-31

  The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.

  本发明涉及吡啶并嗪酮和相关化合物，它们是PARP7的抑制剂，并且在癌症治疗中很有用。
• [EN] 3-OXO-2,6-DIPHENYL-2,3-DIHYDROPYRIDAZINE-4-CARBOXAMIDES<br/>[FR] 3-OXO-2,6-DIPHÉNYL-2,3-DIHYDROPYRIDAZINE-4-CARBOXAMIDES
  申请人：BAYER PHARMA AG

  公开号：WO2017202816A1

  公开（公告）日：2017-11-30

  The present invention covers 3-oxo-2,6-diphenyl-2,3-dihydropyridazine-4-carboxamide compounds of general formula (I): in which R1, R2, R3, R4, R5 and R6 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with 10 dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.

  本发明涵盖了一般式(I)的3-氧代-2,6-二苯基-2,3-二氢吡啶嗪-4-羧酰胺化合物：其中R1、R2、R3、R4、R5和R6如本文所定义，制备所述化合物的方法，用于制备所述化合物的有用中间体化合物，包括所述化合物的药物组合物和组合物，以及利用所述化合物制造用于治疗或预防疾病的药物组合物，特别是癌症或与异常AHR信号传导相关的疾病，或与10种不规则免疫反应或其他与异常AHR信号传导相关的疾病的情况，作为单一药剂或与其他活性成分结合使用。
• Organocatalytic Approach to the Enantioselective Total Synthesis of (+)-Serinolamides A and B and (+)-Lacosamide
  作者：Suresh B. Waghmode、Amardeep R. Jadhao

  DOI：10.1055/a-2222-3822

  日期：2024.5

  A short and highly efficient enantioselective synthesis of (+)-serinolamide A, B and (+)-lacosamide from 3-methoxypropanal using l-proline-catalyzed α-amination, Grubbs metathesis, and acid-amine coupling as key steps is reported.

  使用 3-甲氧基丙醛，短时高效对映选择性合成 (+)-丝氨醇酰胺 A、B 和 (+)-拉科酰胺我据报道，脯氨酸催化的α-氨基化、格拉布斯复分解和酸-胺偶联是关键步骤。
• Discovery of Novel DNA Gyrase Inhibiting Spiropyrimidinetriones: Benzisoxazole Fusion with N-Linked Oxazolidinone Substituents Leading to a Clinical Candidate (ETX0914)
  作者：Gregory S. Basarab、Peter Doig、Vincent Galullo、Gunther Kern、Amy Kimzey、Amy Kutschke、Joseph P. Newman、Marshall Morningstar、John Mueller、Linda Otterson、Karthick Vishwanathan、Fei Zhou、Madhusudhan Gowravaram

  DOI：10.1021/acs.jmedchem.5b00863

  日期：2015.8.13

  A novel class of bacterial type-II topoisomerase inhibitor displaying a spiropyrimidinetrione architecture fused to a benzisoxazole scaffold shows potent activity against Grampositive and fastidious Gram-negative bacteria. Here, we describe a series of N-linked oxazolidinone substituents on the benzisoxazole that improve upon the antibacterial activity of initially described compounds of the class, show favorable PK properties, and demonstrate efficacy in an in vivo Staphylococcus aureus infection model. Inhibition of the topoisomerases DNA gyrase and topoisomerase IV from both Gram-positive and a Gram-negative organisms was demonstrated. Compounds showed a clean in vitro toxicity profile, including no genotoxicity and no bone marrow toxicity at the highest evaluated concentrations or other issues that have been problematic for some fluoroquinolones. Compound lu was identified for advancement into human clinical trials for treatment of uncomplicated gonorrhea based on a variety of beneficial attributes including the potent activity and the favorable safety profile.