2-(bicyclo[2.2.1 ]heptan-2-ylamino)-5-methylthiazol-4(5H)-one | 937187-45-6

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 异戊烯醇脂质
• 英文名称: 2-(bicyclo[2.2.1 ]heptan-2-ylamino)-5-methylthiazol-4(5H)-one
• 英文别名: 2-(bicyclo[2.2.1]heptan-2-ylamino)-5-methylthiazol-4(5H)-one；2-(2-bicyclo[2.2.1]heptanylimino)-5-methyl-1,3-thiazolidin-4-one
• CAS: 937187-45-6
• 化学式: C₁₁H₁₆N₂OS
• 分子量: 224.327
• InChiKey: SIHHTGKQHHWZRM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  66.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-(bicyclo[2.2.1 ]heptan-2-ylamino)-5-methylthiazol-4(5H)-one 、 1-碘代丙烷 在 正丁基锂 、 四甲基乙二胺 、 N¹,N³-bis((R)-1-phenyl-2-(piperidin-1-yl)ethyl)propane-1,3-diamine 作用下， 以 甲苯 为溶剂， 反应 18.25h， 以67.7%的产率得到(5S)-2-((1S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-methyl-5-propylthiazol-4(5H)-one
  参考文献：
  名称：

  WO2009/2445

  摘要：

  公开号：

文献信息

• Catalyzed process of making C-5-substituted heterocyclic inhibitors of 11beta-hydroxy steroid dehydrogenase type 1
  申请人：Bunel Emilio

  公开号：US20070117985A1

  公开（公告）日：2007-05-24

  The invention provides a process for preparing 11 β-hydroxy steroid dehydrogenase type 1 inhibitors of formula 2 via a catalyzed reaction between a compound of formula 1 and a compound of formula R 2 LG in the presence of base: where R 1 , R 2 , X, Y, and LG are described in the specification. Exemplary catalysts contain palladium and one or more phosphine ligands. The process can be performed in a stereoselective manner to give enantiomerically enriched products.

  本发明提供了一种制备11β-羟基类固醇脱氢酶1型抑制剂2的方法，该方法通过在碱存在下，化合物1和化合物R2LG之间催化反应而得到。其中，R1、R2、X、Y和LG在说明书中有描述。示例催化剂包含钯和一个或多个膦配体。该过程可以立体选择性地进行，以得到对映体富集的产物。
• Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
  申请人：Henriksson Martin

  公开号：US20060142357A1

  公开（公告）日：2006-06-29

  The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

  本发明涉及具有式（I），（II），（III）或（IV）的化合物：其中R1，R2，R3，R4，R5，R6，R7，X和Z如本文所定义，并且还涉及包含该化合物的制药组合物，以及使用该化合物治疗与人类11-β-羟基类固醇脱氢酶1型酶相关的疾病和制备作用于人类11-β-羟基类固醇脱氢酶1型酶的药物的方法。
• Inhibitors of 11-β-hydroxy steroid dehydrogenase type 1
  申请人：Amgen, Inc.

  公开号：US07253196B2

  公开（公告）日：2007-08-07

  The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

  本发明涉及公式（I），（II），（III）或（IV）的化合物： 其中R1，R2，R3，R4，R5，R6，R7，X和Z如定义所述，并且还涉及包含该化合物的制药组合物，以及使用该化合物治疗与人类11-β-羟基类固醇脱氢酶类型1酶相关的疾病的方法，以及用于制备作用于人类11-β-羟基类固醇脱氢酶类型1酶的药物。
• Inhibitors of 11-Beta-Hydroxy Steroid Dehydrogenase Type 1
  申请人：Henriksson Martin

  公开号：US20070281938A1

  公开（公告）日：2007-12-06

  The present invention relates to compounds with the formula (I) wherein R 1 , R 2 , R 3 , R 4 , and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

  本发明涉及化合物式（I），其中R1、R2、R3、R4和Z的定义如本文所述，以及包含该化合物的制药组合物，以及该化合物在医学上的使用和用于制备对人类11-β-羟基类固醇脱氢酶1型酶起作用的药物。
• Catalyzed process of making C-5-substituted heterocyclic inhibitors of 11β-hydroxy steroid dehydrogenase type 1
  申请人：Amgen Inc.

  公开号：US07541474B2

  公开（公告）日：2009-06-02

  The invention provides a process for preparing 11 β-hydroxy steroid dehydrogenase type 1 inhibitors of formula 2 via a catalyzed reaction between a compound of formula 1 and a compound of formula R2LG in the presence of base: where R1, R2, X, Y, and LG are described in the specification. Exemplary catalysts contain palladium and one or more phosphine ligands. The process can be performed in a stereoselective manner to give enantiomerically enriched products.

  该发明提供了一种制备11β-羟基类固醇脱氢酶1型抑制剂的方法，该方法通过在碱存在下，化合物1和化合物R2LG之间的催化反应制备公式2的产物，其中R1、R2、X、Y和LG在说明书中描述。示例催化剂包含钯和一个或多个膦配体。该过程可以立体选择性地进行，以给出对映体富集的产物。