Tert-butyl 4-hydroxy-4-[2-(methoxymethoxy)phenyl]piperidine-1-carboxylate | 932372-91-3

• 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: Tert-butyl 4-hydroxy-4-[2-(methoxymethoxy)phenyl]piperidine-1-carboxylate
• CAS: 932372-91-3
• 化学式: C₁₈H₂₇NO₅
• 分子量: 337.416
• InChiKey: NMRRKEGWAVJALT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  24
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  68.2
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  Tert-butyl 4-hydroxy-4-[2-(methoxymethoxy)phenyl]piperidine-1-carboxylate 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 18.0h， 生成 2-(1,2,3,6-Tetrahydropyridin-4-yl)phenol
  参考文献：
  名称：

  WO2007/37187

  摘要：

  公开号：
• 作为产物：
  描述：

  1-溴-2-(甲氧基甲氧基)苯 、 N-叔丁氧羰基-4-哌啶酮 在 正丁基锂 作用下， 以 四氢呋喃 、 正己烷 为溶剂， 反应 1.17h， 以19%的产率得到Tert-butyl 4-hydroxy-4-[2-(methoxymethoxy)phenyl]piperidine-1-carboxylate
  参考文献：
  名称：

  WO2007/37187

  摘要：

  公开号：

文献信息

• DIARYLETHER DERIVATIVES AS ANTITUMOR AGENTS
  申请人：Matsuyama Hironori

  公开号：US20100004438A1

  公开（公告）日：2010-01-07

  An object of the present invention is to provide a medicinal drug much improved in anti tumor activity and excellent in safety. According to the present invention, there is provided a medicinal drug containing a compound represented by the following general formula (1) or a salt thereof as an active ingredient: [Formula 1] wherein X 1 represents a nitrogen atom or a group —CH═, R 1 represents a group -Z-R 6 , in which Z represents a group —CO—, a group —CH(OH)— or the like, R 6 represents a 5- to 15-membered monocyclic, dicyclic or tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, R 2 represents a hydrogen atom or a halogen atom, Y represents a group —O—, a group —CO—, a group —CH(OH)— or a lower alkylene group, and A represents [Formula 2] wherein R 3 represents a hydrogen atom, a lower alkoxy group or the like, p represents 1 or 2, R 4 represents an imidazolyl lower alkyl group or the like.

  本发明的一个目的是提供一种在抗肿瘤活性方面大大改进且安全性优异的药物。根据本发明，提供了一种包含以下一般式（1）所表示的化合物或其盐作为活性成分的药物：[式1]其中X1代表氮原子或基团—CH═，R1代表一个基团-Z-R6，其中Z代表基团—CO—，基团—CH(OH)—或类似的基团，R6代表一个含有1至4个氮原子、氧原子或硫原子的5至15个成员的单环、双环或三环饱和或不饱和杂环基团，R2代表氢原子或卤原子，Y代表基团—O—，基团—CO—，基团—CH(OH)—或低碳烷基基团，A代表[式2]其中R3代表氢原子、低碳氧基基团或类似基团，p代表1或2，R4代表咪唑基低碳基团或类似基团。
• Aromatic Compounds
  申请人：Fukushima Tae

  公开号：US20070270422A1

  公开（公告）日：2007-11-22

  The present invention provides a novel compound, which has an excellent effect of suppressing the generation of collagen and less side effects, with being excellent in terms of safety. The compound of the present invention is represented by the following general formula (1): [wherein X 1 represents a nitrogen atom or a group —CH═; R 1 represents a group -Z-R 6 , wherein Z represents a group —CO—, a group —CH(OH)—, or the like, and R 6 represents a 5- to 15-membered monocyclic, dicyclic, or tricyclic, saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms, or sulfur atoms; R 2 represents a hydrogen atom, a halogen atom or a lower alkylene group; Y represents a group —O—, a group —CO—, a group —CH(OH)—, a lower alkylene group, or the like; and A represents a group or the like, wherein R 3 represents a hydrogen atom, a lower alkoxy group, or the like, p represents 1 or 2, and R 4 represents an imidazolyl lower alkyl group or the like.

  本发明提供了一种新型化合物，具有抑制胶原生成的优异效果，并且具有较少的副作用，在安全性方面表现出色。本发明的化合物由以下通式（1）表示：[其中X1代表氮原子或基团—CH═；R1代表基团-Z-R6，其中Z代表基团—CO—、基团—CH(OH)—或类似基团，而R6代表具有1到4个氮原子、氧原子或硫原子的5-到15元的单环、双环或三环、饱和或不饱和杂环基团；R2代表氢原子、卤素原子或低碳链基团；Y代表基团—O—、基团—CO—、基团—CH(OH)—、低碳链基团或类似基团；A代表基团或类似基团，其中R3代表氢原子、低碳醚基团或类似基团，p代表1或2，而R4代表咪唑基低碳基团或类似基团。
• AROMATIC COMPOUND
  申请人：FUKUSHIMA Tae

  公开号：US20120238750A1

  公开（公告）日：2012-09-20

  The compound of the present invention is represented by the following general formula (1): [wherein X 1 represents a nitrogen atom or a group —CH═; R 1 represents a group —Z—R 6 , wherein Z represents a group —CO—, a group —CH(OH)—, or the like, and R 6 represents a 5- to 15-membered monocyclic, dicyclic, or tricyclic, saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms, or sulfur atoms; R 2 represents a hydrogen atom, a halogen atom or a lower alkylene group; Y represents a group —O—, a group —CO—, a group —CH(OH)—, a lower alkylene group, or the like; and A represents a group or the like, wherein R 3 represents a hydrogen atom, a lower alkoxy group, or the like, p represents 1 or 2, and R 4 represents an imidazolyl lower alkyl group or the like.

  本发明的化合物由以下通式（1）表示：[其中X1表示氮原子或基团—CH═; R1表示基团—Z—R6，其中Z表示基团—CO—、基团—CH（OH）—或类似物，而R6表示具有1至4个氮原子、氧原子或硫原子的5至15环的单环、双环或三环、饱和或不饱和的杂环基团; R2表示氢原子、卤素原子或较低的烷基链; Y表示基团—O—、基团—CO—、基团—CH（OH）—、较低的烷基链或类似物; A表示基团或类似物，其中R3表示氢原子、较低的烷氧基或类似物，p表示1或2，而R4表示咪唑基较低的烷基链或类似物。
• SULFONAMIDE DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONISTIC ACTIVITY
  申请人：Shionogi&Co., Ltd.

  公开号：EP1939175A1

  公开（公告）日：2008-07-02

  The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (II): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.; a pharmaceutically acceptable salt or a hydrate thereof.

  本发明提供了一种具有DP受体拮抗活性的磺酰胺衍生物和一种包含上述化合物作为活性成分的药物组合物，并进一步提供了一种治疗过敏性疾病的治疗剂。 通式(II)的化合物： 其中环 A 是芳香碳环等；环 B 是含氮非芳香杂环等；环 C 是芳香碳环等；R1 是羧基等；R2 独立地是卤素原子等；R3 是任选取代的烷氧基等；R4 独立地是卤素原子等；R5 独立地是任选取代的烷基等；M 是磺酰基等。M是磺酰基等；Y是单键等；L1是单键等；L2是单键等；k是0、1、2、3或4；n是0、1或2；q是0、1、2或3；条件是 a) 当环 B 是含有一个或两个氮原子的 6 元含氮杂环且环 C 是苯环等时，k 不是 0； 药学上可接受的盐或其水合物。
• PGD2 receptor antagonist
  申请人：Shionogi & Co., Ltd.

  公开号：EP2407453A1

  公开（公告）日：2012-01-18

  A compound of the general formula (I) for use in the treatment of diseases associated with a PGD2 receptor: wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is hydroxyalkyl etc.; R2 is independently a halogen atom etc.; R3 is a hydrogen atom etc.; R4 is independently a halogen atom etc.; R5 is independently a halogen atom etc.; M is carbonyl etc.; Y is a single bond etc.; L1, L2 and L3 are independently a single bond etc.; R6 and R7 are independently a hydrogen atom etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s), and the ring C is a benzene ring, b) the ring C is not an indole ring or an azaindole ring, c) R1 is not carboxy when the ring C is a benzene ring, -L3- is - (O-alkylene)-, and the substituting position of L3 and Y is an ortho-position each other in the ring C, and d) the substituting position of L3 and Y is not a para-position in the ring C when the ring B is a thiazolidine ring and the ring C is a benzene ring; a pharmaceutically acceptable salt or solvate thereof.

  用于治疗与 PGD2 受体相关疾病的通式 (I) 化合物： 其中，环 A 是芳香碳环等；环 B 是含氮非芳香杂环等；环 C 是芳香碳环等；R1 是羟烷基等；R2 独立地是卤素原子等；R3 是氢原子等；R4 独立地是卤素原子等；R5 独立地是卤素原子等。R3 是氢原子等；R4 独立地是卤素原子等；R5 独立地是卤素原子等；M 是羰基等；Y 是单键等；L1、L2 和 L3 独立地是单键等；R6 和 R7 独立地是氢原子等。k 为 0、1、2、3 或 4；n 为 0、1 或 2；q 为 0、1、2 或 3；条件是：a) 当环 B 是含有一个或两个氮原子的 6 元含氮杂环且环 C 是苯环时，k 不是 0；b) 环 C 不是吲哚环或氮杂吲哚环；c) 当环 C 是苯环时，R1 不是羧基、-当环 B 是噻唑烷环而环 C 是苯环时，-L3- 是-(O-烯烃)-，并且 L3 和 Y 的取代位置在环 C 中互为正交位置，以及 d) L3 和 Y 的取代位置在环 C 中不是对位； 其药学上可接受的盐或溶液。