1-acetoxy-3-morpholin-4-yl-propan-2-ol | 51735-25-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 1-acetoxy-3-morpholin-4-yl-propan-2-ol
• 英文别名: (2-Hydroxy-3-morpholin-4-ylpropyl) acetate
• CAS: 51735-25-2
• 化学式: C₉H₁₇NO₄
• 分子量: 203.238
• InChiKey: RLDIHYQYIYJARP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.8
• 重原子数：
  14
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  59
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  3-(4-吗啉基)-1,2-丙二醇 、 1-乙酰基咪唑 在 四甲基氢氧化铵 作用下， 以 水 为溶剂， 反应 16.08h， 以55%的产率得到1-acetoxy-3-morpholin-4-yl-propan-2-ol
  参考文献：
  名称：

  四甲基氢氧化铵在水中催化碳水化合物和二醇的区域选择性乙酰化

  摘要：

  描述了一种用于在水溶液中有效地对碳水化合物和二醇进行区域选择性乙酰化的新方法。在温和的条件下，在水中用1-乙酰基咪唑和氢氧化四甲基铵（TMAH）处理底物，可得到伯羟基的高度区域选择性乙酰化。该发现为水中非保护的糖苷和二醇的选择性乙酰化提供了一种环保的方法，避免了使用有毒有机溶剂和避免对仲羟基进行预保护的必要性。

  DOI：

  10.1039/c4gc00770k

文献信息

• NICOTINAMIDES AS JAK KINASE MODULATORS
  申请人：Bauer Shawn M.

  公开号：US20120108566A1

  公开（公告）日：2012-05-03

  The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

  本发明涉及具有公式I的化合物及其药用可接受的盐、酯和前药，这些化合物是JAK激酶的抑制剂。本发明还涉及用于制备这类化合物的中间体，该化合物的制备，含有该化合物的药物组合物，抑制JAK激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗至少部分由JAK激酶活性介导的多种疾病条件的方法，例如不良血栓形成和非霍奇金淋巴瘤。
• [EN] 2, 6-DIAMINO-PYRIMIDIN- 5-YL-CARBOXAMIDES AS SYK OR JAK KINASES INHIBITORS<br/>[FR] 2, 6-DIAMINO-PYRIMIDIN- B-YL-CARBOXAMIDES SERVANT D'INHIBITEURS DE Syk KINASES ET DE JANUS KINASES
  申请人：PORTOLA PHARM INC

  公开号：WO2009145856A1

  公开（公告）日：2009-12-03

  The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as cardiovascular disease, inflammatory disease, autoimmune disease and cell proliferative disorder, thrombosis, allergy, asthma, rheumatoid arthritis, leukemia, or non-Hodgkin's lymphoma.

  本发明涉及式I-II的化合物及其药学上可接受的互变异构体、盐或立体异构体，这些化合物是syk和/或JAK激酶的抑制剂。本发明还涉及用于制备这类化合物的中间体，制备这种化合物，含有这种化合物的药物组合物，抑制syk和/或JAK激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗由syk和/或JAK激酶活性至少部分介导的多种疾病的方法，如心血管疾病、炎症性疾病、自身免疫疾病和细胞增殖障碍、血栓形成、过敏、哮喘、类风湿关节炎、白血病或非霍奇金淋巴瘤。
• [EN] OXYPYRIMIDINES AS SYK MODULATORS<br/>[FR] OXYPYRIMIDINES EN TANT QUE MODULATEURS DE SYK
  申请人：PORTOLA PHARM INC

  公开号：WO2012061415A1

  公开（公告）日：2012-05-10

  The present invention is directed to compounds of formula (I) and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which arc inhibitor of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

  本发明涉及式(I)的化合物及其互变异构体或药用可接受的盐、酯和前药，其为Syk激酶的抑制剂。本发明还涉及用于制备这种化合物的中间体，该化合物的制备，含有该化合物的药物组合物，抑制Syk激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗至少部分由Syk激酶活性介导的多种疾病的方法，如不良血栓形成和非霍奇金淋巴瘤。
• [EN] DEXAMETHASONE COMBINATION THERAPY<br/>[FR] POLYTHÉRAPIE À LA DEXAMÉTHASONE
  申请人：UNIV TEXAS

  公开号：WO2012065021A1

  公开（公告）日：2012-05-18

  The present invention relates to a method of treating multiple myeloma in a subject comprising administering to the subject an amount of (1) a compound of formula (I), as described herein, and/or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, and an amount of (2) dexamethasone and/or a pharmaceutically acceptable salt, solvate, metabolite or racemate thereof, such that the subject is treated. In another aspect, provided herein is a method of treating multiple myeloma in a subject comprising administering to the subject an amount of (1) a compound of formula (I) and an amount of (2) dexamethasone, such that the subject is treated; pharmaceutical formulations comprising said combination for the treatment of multiple myelom; and compositions thereof.

  本发明涉及一种治疗多发性骨髓瘤的方法，包括向受试者注射(1)公式(I)所述的化合物和/或其立体异构体、互变异构体或药学上可接受的盐，以及(2)地塞米松和/或其药学上可接受的盐、溶剂、代谢物或外消旋体的剂量，以使受试者得到治疗。在另一方面，本发明提供了一种治疗多发性骨髓瘤的方法，包括向受试者注射(1)公式(I)的化合物和(2)地塞米松的剂量，以使受试者得到治疗；以及用于治疗多发性骨髓瘤的该组合的制剂和组成物。
• DEXAMETHASONE COMBINATION THERAPY
  申请人：Yi Qing

  公开号：US20130310352A1

  公开（公告）日：2013-11-21

  The present invention relates to a method of treating multiple myeloma in a subject comprising administering to the subject an amount of (1) a compound of formula (I), as described herein, and/or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, and an amount of (2) dexamethasone and/or a pharmaceutically acceptable salt, solvate, metabolite or racemate thereof, such that the subject is treated. In another aspect, provided herein is a method of treating multiple myeloma in a subject comprising administering to the subject an amount of (1) a compound of formula (I) and an amount of (2) dexamethasone, such that the subject is treated; pharmaceutical formulations comprising said combination for the treatment of multiple myelom; and compositions thereof.

  本发明涉及一种治疗多发性骨髓瘤的方法，包括向患者施用（1）公式（I）所述的化合物及/或其立体异构体，互变异构体或其药学上可接受的盐的量，以及（2）地塞米松和/或其药学上可接受的盐，溶剂，代谢物或外消旋体的量，从而治疗患者。在另一个方面，本发明提供了一种治疗多发性骨髓瘤的方法，包括向患者施用（1）公式（I）的化合物的量和（2）地塞米松的量，从而治疗患者；用于治疗多发性骨髓瘤的上述组合物的药物制剂；以及它们的组成物。