2-amino-1-morpholinylpropyl-1-one | 124491-97-0

• 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: 2-amino-1-morpholinylpropyl-1-one
• 英文别名: 4-Alanyl-morpholin；4-alanyl-morpholine；4-DL-alanyl-morpholine；4-DL-Alanyl-morpholin；2-Amino-1-(4-morpholinyl)-1-propanone；2-amino-1-morpholin-4-ylpropan-1-one
• CAS: 124491-97-0
• 化学式: C₇H₁₄N₂O₂
• mdl: MFCD09927761
• 分子量: 158.2
• InChiKey: SLVJYKCZTXDMFR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.857
• 拓扑面积：
  55.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-amino-1-morpholinylpropyl-1-one 、 长春乙酯羧酸 在 2-(7-azobenzotriazole)-N,N,N’,N’-tetramethyluronium hexafluorophosphate 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 15.0h， 以30.51%的产率得到(4¹S,13aS)-13a-ethyl-N-(1-morpholinyl-1-oxopropyl-2-yl)-2,3,4¹,5,6,13a-hexahydro-1H-indolo[3,2,1-de]pyrido[3,2,1-ij][1,5]naphthyridin-12-carboxamide
  参考文献：
  名称：

  DIAZA-BENZOFLUORANTHRENE COMPOUNDS

  摘要：

  揭示了一系列二氮杂苯并芴类化合物。本发明特别涉及一种由式(I)表示的化合物，其药学上可接受的盐或互变异构体。

  公开号：

  US20180016270A1
• 作为产物：
  描述：

  tert-butyl (1-morpholinyl-1-oxopropan-2-yl)carbamate 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 2.0h， 以72.66%的产率得到2-amino-1-morpholinylpropyl-1-one
  参考文献：
  名称：

  DIAZA-BENZOFLUORANTHRENE COMPOUNDS

  摘要：

  揭示了一系列二氮杂苯并芴类化合物。本发明特别涉及一种由式(I)表示的化合物，其药学上可接受的盐或互变异构体。

  公开号：

  US20180016270A1

文献信息

• [EN] [1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINES<br/>[FR] [1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINES
  申请人：BAYER AG

  公开号：WO2021028382A1

  公开（公告）日：2021-02-18

  The present invention covers [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds of general formula (I) in which R1, R2, R3, R4, R5, R6, R7 and R8 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.

  本发明涵盖了通式（I）中R1、R2、R3、R4、R5、R6、R7和R8如所定义的[1,2,4]三唑并[1,5-c]喹唑啉-5-胺化合物，以及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有关的情况，作为唯一药剂或与其他活性成分组合使用。
• [EN] SUBSTITUTED PYRROLOPYRIDINE-DERIVATIVES<br/>[FR] DÉRIVÉS DE PYRROLOPYRIDINE SUBSTITUÉS
  申请人：BAYER PHARMA AG

  公开号：WO2018228920A1

  公开（公告）日：2018-12-20

  The present invention relates to protein-inhibitory substituted pyrrolopyridine derivatives of formula (I) in which X, Y, R1, R2, R3 and R4 are as defined herein, to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, repectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients. The present invention further relates to the use, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control.

  本发明涉及公式（I）中X、Y、R1、R2、R3和R4如本文所定义的蛋白抑制取代吡咯吡啶衍生物，涉及包含根据本发明的化合物的药物组合物和制剂，以及创新化合物的预防和治疗用途，分别用于制造用于治疗或预防疾病的药物组合物，特别是用于恶性肿瘤障碍，癌症或与MAP4K1信号异常相关的其他疾病，作为唯一药剂或与其他活性成分组合使用。本发明还涉及用途，分别用于制造药物组合物，用于治疗或预防良性增生中的蛋白酶抑制剂，在动脉粥样硬化疾病、败血症、自身免疫疾病、血管疾病、病毒感染、神经退行性疾病、炎症性疾病、动脉粥样硬化疾病和男性生育控制方面。
• Studies concerning the antibiotic actinonin. Part III. Synthesis of structural analogues of actinonin by the anhydride–imide method
  作者：John P. Devlin、W. David Ollis、John E. Thorpe、Ronald J. Wood、Barbara J. Broughton、Peter J. Warren、Kenneth R. H. Wooldridge、Derek E. Wright

  DOI：10.1039/p19750000830

  日期：——

  A synthetic route, associated with a high degree of stereoselectivity, has been developed for the synthesis of structural analogues (XIII) of actinonin (I). The anhydride–imide method involves the sequence (IIIb)+(V)→[(VI)+(VII)]→(XI)→(XIII). (±)-Amino-amides (IIIb) yielded the (±)-hydroxamic acids with the relative configuration (XIII) and L-amino-amides (X) yielded single enantiomers with the absolute

  已经开发了具有高度立体选择性的合成路线，用于合成肌动蛋白（I）的结构类似物（XIII）。酸酐-酰亚胺法涉及序列（IIIb）+（V）→ [（VI）+（VII）] →（XI）→（XIII）。（±）-氨基酰胺（IIIb）产生具有相对构型（XIII）的（±）-异羟肟酸，并且L-氨基酰胺（X）产生具有绝对构型（XIII）的单一对映体。
• Substituted pyrazole derivatives and related compounds as bradykinin B1 receptor antagonists
  申请人：Tung S. Jay

  公开号：US20050038099A1

  公开（公告）日：2005-02-17

  Disclosed are compounds that are bradykinin B 1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B 1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action.

  本发明涉及一种是Bradykinin B1受体拮抗剂的化合物，可用于治疗哺乳动物中由Bradykinin B1受体介导的疾病或缓解与疾病状况相关的不良症状。其中某些化合物表现出增强的效力，并且预计还会表现出持续时间的增加。
• 4-Bromo-5-(2-chloro-benzoylamino)-1h-pyrazole-3-carboxylic acid (1-aminocarbonyl)eth-1-yl) amide derivatives and related compounds as bradykinin b1 receptor antagonists for the treatment of inflammatory diseases
  申请人：Tung S. Jay

  公开号：US20070161633A1

  公开（公告）日：2007-07-12

  Disclosed are compounds of formulae (I) and (II) that are bradykinin B 1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B 1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action. Wherein Z is selected from O, S and NH; Q of formula (III) and the other substituents are as defined in claim 1.

  本发明涉及式(I)和(II)的化合物，它们是布雷地奎宁B1受体拮抗剂，可用于治疗哺乳动物中由布雷地奎宁B1受体介导的疾病或缓解与疾病状况相关的不良症状。其中Z从O、S和NH中选择；公式(III)中的Q和其他取代基如权利要求1所定义。其中某些化合物表现出增强的效力，并且预计还会表现出延长作用时间。