1-tert-butoxycarbonyl-3-phenyl-4-hydroxypiperidine | 632352-57-9

• 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: 1-tert-butoxycarbonyl-3-phenyl-4-hydroxypiperidine
• 英文别名: tert-Butyl (3R*,4S*)-4-hydroxy-3-phenylpiperidine-1-carboxylate；4-hydroxy-3-phenylpiperidine-1-carboxylic acid tert-butyl ester；tert-Butyl 4-hydroxy-3-phenyl-1-piperidinecarboxylate；tert-butyl 4-hydroxy-3-phenylpiperidine-1-carboxylate
• CAS: 632352-57-9
• 化学式: C₁₆H₂₃NO₃
• 分子量: 277.364
• InChiKey: DISTZHMQLVYZLN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  49.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-nitro-5-(trifluoromethyl)benzyl methanesulfonate 、 1-tert-butoxycarbonyl-3-phenyl-4-hydroxypiperidine 在 sodium hydroxide 、 水 、 四丁基硫酸氢铵 、 sodium iodide 作用下， 以 二氯甲烷 为溶剂， 反应 12.0h， 生成 cis-4-[[3-nitro-5-(trifluoromethyl)benzyl]oxy]-3-phenylpiperidine
  参考文献：
  名称：

  EP1553084

  摘要：

  公开号：
• 作为产物：
  描述：

  1-Boc-3-苯基哌啶-4-酮 在 L-Selectride 作用下， 以 四氢呋喃 为溶剂， 反应 1.0h， 以95%的产率得到1-tert-butoxycarbonyl-3-phenyl-4-hydroxypiperidine
  参考文献：
  名称：

  EP1553084

  摘要：

  公开号：

文献信息

• Novel piperidyl derivatives of quinazoline and isoquinoline
  申请人：Humphrey Michael John

  公开号：US20060019975A1

  公开（公告）日：2006-01-26

  The invention pertains to new piperidyl-substituted quinazoline and isoquinoline derivatives that serve as effective phosphodiesterase (PDE) inhibitors. The invention also relates to compounds that are selective inhibitors of PDE10. The invention further relates to intermediates for preparation of such compounds; pharmaceutical compositions comprising such compounds; and the use of such compounds in methods for treating certain central nervous system (CNS) or other disorders.

  本发明涉及新的哌啶基取代的喹唑啉和异喹啉衍生物，可作为有效的磷酸二酯酶（PDE）抑制剂。本发明还涉及选择性抑制剂PDE10的化合物。本发明还涉及用于制备这类化合物的中间体；包含这类化合物的药物组合物；以及利用这类化合物治疗某些中枢神经系统（CNS）或其他疾病的方法。
• NK1 and NK3 antagonists
  申请人：O'Neill T. Brian

  公开号：US20050256164A1

  公开（公告）日：2005-11-17

  The invention is to a compound exhibiting neurokinin inhibitory properties, a pharmaceutical composition comprising same and a method of treatment for neurokinin-mediated conditions.

  这项发明涉及一种具有神经激肽抑制性能的化合物，包括该化合物的药物组合物以及用于神经激肽介导疾病的治疗方法。
• Piperidine derivative, process for producing the same, and use
  申请人：Ikeura Yoshinori

  公开号：US20060167052A1

  公开（公告）日：2006-07-27

  The present invention provides a compound represented by the formula: wherein Ar is an aryl group, an aralkyl group or an aromatic heterocyclic group, each of which may be substituted, R 1 is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group, X is an oxygen atom or an optionally lo substituted imino group, Z is an optionally substituted methylene group, Ring A is an optionally further substituted piperidine ring, and Ring B is an optionally substituted aromatic ring, provided that when Z is a methylene group substituted with an oxo group, R 1 is not a methyl group, and 15 when Z is a methylene group substituted with a methyl group, Ring B is a substituted aromatic ring, or a salt thereof, which is a novel piperidine derivative having excellent antagonistic action for a tachykinin receptor and useful as a medicament, particularly an agent for preventing and/or treating urinary frequency and/or urinary incontinence.

  本发明提供了一种化合物，其表示为以下式子：其中Ar是芳基、芳基烷基或芳香杂环基，每个基团都可以被取代，R1是氢原子、可选取代的碳氢基团、酰基或可选取代的杂环基团，X是氧原子或可选取代的亚胺基团，Z是可选取代的亚甲基团，环A是可选进一步取代的哌啶环，环B是可选取代的芳香环，但当Z是取代有氧基的亚甲基团时，R1不是甲基基团，而当Z是取代有甲基基团的亚甲基团时，环B是取代的芳香环，或其盐。该化合物是一种新型哌啶衍生物，具有优异的缓解速激肽受体拮抗作用，可用作药物，特别是用作预防和/或治疗尿频和/或尿失禁的药剂。
• PIPERIDINE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1553084A1

  公开（公告）日：2005-07-13

  The present invention provides a compound represented by the formula:    wherein Ar is an aryl group, an aralkyl group or an aromatic heterocyclic group, each of which may be substituted, R1 is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group, X is an oxygen atom or an optionally substituted imino group, Z is an optionally substituted methylene group, Ring A is an optionally further substituted piperidine ring, and Ring B is an optionally substituted aromatic ring, provided that when Z is a methylene group substituted with an oxo group, R1 is not a methyl group, and when Z is a methylene group substituted with a methyl group, Ring B is a substituted aromatic ring, or a salt thereof, which is a novel piperidine derivative having excellent antagonistic action for a tachykinin receptor and useful as a medicament, particularly an agent for preventing and/or treating urinary frequency and/or urinary incontinence.

  本发明提供了一种由式表示的化合物： 其中 Ar 是芳基、芳烷基或芳香杂环基团，每个基团均可被取代；R1 是氢原子、任选取代的烃基、酰基或任选取代的杂环基团；X 是氧原子或任选取代的亚氨基；Z 是任选取代的亚甲基；环 A 是任选进一步取代的哌啶环；环 B 是任选取代的芳香环、当 Z 是被氧代基团取代的亚甲基时，R1 不是甲基；当 Z 是被甲基取代的亚甲基时，环 B 是被取代的芳香环，或其盐，这是一种新型哌啶衍生物，对快速激肽受体有很好的拮抗作用，可用作药物，特别是预防和/或治疗尿频和/或尿失禁的药物。
• Piperidinyl-3-(aryloxy)propanamides and propanoates
  申请人：Takeda Pharmaceutical Company Limited

  公开号：US11045457B2

  公开（公告）日：2021-06-29

  Disclosed are compounds of Formula 1, stereoisomers thereof, and pharmaceutically acceptable salts thereof, wherein L, r, s, R5, R6, R7, R9, R10, R11, R12, X1, X2, X3, X4, X13, and X14 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with SSTR4.

  公开了式 1 的化合物、 其中 L、r、s、R5、R6、R7、R9、R10、R11、R12、X1、X2、X3、X4、X13 和 X14 在说明书中定义。本公开还涉及制备式 1 化合物的材料和方法、含有它们的药物组合物，以及它们在治疗与 SSTR4 相关的疾病、失调和病症方面的用途。