methyl 2-(1-(tert-butoxycarbonyl)piperidin-4-yl)-2,5-dihydrooxazole-4-carboxylate | 1238759-94-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: methyl 2-(1-(tert-butoxycarbonyl)piperidin-4-yl)-2,5-dihydrooxazole-4-carboxylate
• 英文别名: Methyl 2-[1-[(2-methylpropan-2-yl)oxycarbonyl]piperidin-4-yl]-2,5-dihydro-1,3-oxazole-4-carboxylate
• CAS: 1238759-94-8
• 化学式: C₁₅H₂₄N₂O₅
• 分子量: 312.366
• InChiKey: ILNDZWDLRUEJDT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  22
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  77.4
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  methyl 2-(1-(tert-butoxycarbonyl)piperidin-4-yl)-2,5-dihydrooxazole-4-carboxylate 在 N-溴代丁二酰亚胺(NBS) 、 potassium carbonate 作用下， 以 1,2-二氯乙烷 为溶剂， 反应 1.25h， 以76%的产率得到methyl 2-(1-(tert-butoxycarbonyl)piperidin-4-yl)oxazole-4-carboxylate
  参考文献：
  名称：

  使用3-恶唑啉-4-羧酸酯为中间体从醛轻松制备恶唑-4-羧酸酯和4-酮

  摘要：

  开发了一种由醛类新的两步合成恶唑-4-羧酸酯的方法，其特征是利用3-恶唑啉-4-羧酸酯作为合成中间体。还描述了基于3-恶唑啉-4-羧酸酯对格氏试剂的有趣反应性，可轻松制备4-酮-恶唑衍生物的方法。

  DOI：

  10.1021/ol1012789
• 作为产物：
  描述：

  L-丝氨酸甲酯盐酸盐 、 1-叔丁氧羰基哌啶-4-甲醛 在 三乙烯二胺 、 N-氯代丁二酰亚胺 作用下， 以 二氯甲烷 为溶剂， 反应 0.6h， 以84%的产率得到methyl 2-(1-(tert-butoxycarbonyl)piperidin-4-yl)-2,5-dihydrooxazole-4-carboxylate
  参考文献：
  名称：

  使用3-恶唑啉-4-羧酸酯为中间体从醛轻松制备恶唑-4-羧酸酯和4-酮

  摘要：

  开发了一种由醛类新的两步合成恶唑-4-羧酸酯的方法，其特征是利用3-恶唑啉-4-羧酸酯作为合成中间体。还描述了基于3-恶唑啉-4-羧酸酯对格氏试剂的有趣反应性，可轻松制备4-酮-恶唑衍生物的方法。

  DOI：

  10.1021/ol1012789

文献信息

• DIAZANAPHTHALEN-3-YL CARBOXAMIDES AND PREPARATION AND USE THEREOF
  申请人：Samumed, LLC

  公开号：US20190127370A1

  公开（公告）日：2019-05-02

  Diazanaphthalene compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a diazanaphthalene compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, inflammation, auto-immune diseases and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.

  本公开涉及使用二氮萘化合物或其类似物治疗通过激活Wnt途径信号传导特征的疾病的方法。更具体地，本公开涉及在治疗由Wnt途径信号传导激活所特征化的疾病（例如癌症、异常细胞增殖、血管生成、阿尔茨海默病、肺部疾病、炎症、自身免疫疾病和骨关节炎）中使用二氮萘化合物或其类似物，以及调节由Wnt途径信号传导介导的细胞事件，以及与DYRK1A过表达相关的神经病症/紊乱/疾病。
• 6-(6-MEMBERED HETEROARYL & ARYL)ISOQUINOLIN-3-YL CARBOXAMIDES AND PREPARATION AND USE THEREOF
  申请人：Samumed, LLC

  公开号：US20190125740A1

  公开（公告）日：2019-05-02

  Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, inflammation, auto-immune diseases and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.

  揭示了用于治疗各种疾病和病理的异喹啉化合物。更具体地，本公开涉及使用异喹啉化合物或其类似物治疗由Wnt途径信号激活所特征的疾病（例如癌症、异常细胞增殖、血管生成、阿尔茨海默病、肺部疾病、炎症、自身免疫疾病和骨关节炎），调节由Wnt途径信号介导的细胞事件，以及与DYRK1A过表达相关的神经状况/疾病/疾病。
• [EN] HETEROARYL DERIVATIVES AS SEPIAPTERIN REDUCTASE INHIBITORS<br/>[FR] DÉRIVÉS D'HÉTÉROARYLE À UTILISER EN TANT QU'INHIBITEURS DE SÉPIAPTÉRINE RÉDUCTASE
  申请人：QUARTET MEDICINE INC

  公开号：WO2017059191A1

  公开（公告）日：2017-04-06

  Inhibitors of sepiapterin reductase of formula (I) or (I'), wherein the substituents are defined as in the claims, and uses of sepiapterin reductase inhibitors in analgesia, treatment of acute and chronic pain, anti-inflammation, and immune cell regulation are disclosed.

  式(I)或(I')的色氨酰还原酶抑制剂，其中取代基如权利要求中所定义，以及这些色氨酰还原酶抑制剂在镇痛、治疗急慢性疼痛、抗炎和免疫细胞调节中的用途被公开。
• 6-(6-membered heteroaryl and aryl)isoquinolin-3-yl carboxamides and preparation and use thereof
  申请人：Samumed, LLC

  公开号：US10653688B2

  公开（公告）日：2020-05-19

  Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, inflammation, auto-immune diseases and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.

  本发明公开了用于治疗各种疾病和病理的异喹啉化合物。更具体地说，本公开涉及异喹啉化合物或其类似物在治疗以 Wnt 通路信号激活为特征的疾病（如癌症、异常细胞增殖、血管生成、阿尔茨海默病、肺病、炎症、自身免疫性疾病和骨关节炎）、调节由 Wnt 通路信号介导的细胞事件以及与 DYRK1A 过度表达相关的神经系统状况/紊乱/疾病中的用途。
• Diazanaphthalen-3-yl carboxamides and preparation and use thereof
  申请人：Samumed, LLC

  公开号：US10703748B2

  公开（公告）日：2020-07-07

  Diazanaphthalene compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a diazanaphthalene compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, inflammation, auto-immune diseases and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.

  本发明公开了用于治疗各种疾病和病理的重氮萘化合物。更具体地说，本公开涉及重氮萘化合物或其类似物在治疗以 Wnt 通路信号激活为特征的疾病（如癌症、异常细胞增殖、血管生成、阿尔茨海默病、肺病、炎症、自身免疫性疾病和骨关节炎）、调节由 Wnt 通路信号介导的细胞事件以及与 DYRK1A 过度表达相关的神经系统状况/紊乱/疾病中的用途。