1-benzyloxycarbonyl-4-hydroxypiperidine-4-carboxylic acid | 67117-20-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-benzyloxycarbonyl-4-hydroxypiperidine-4-carboxylic acid
• 英文别名: N-benzyloxycarbonyl-4-hydroxypiperidine-4-carboxylic acid；1-[(Benzyloxy)carbonyl]-4-hydroxypiperidine-4-carboxylic acid；4-hydroxy-1-phenylmethoxycarbonylpiperidine-4-carboxylic acid
• CAS: 67117-20-8
• 化学式: C₁₄H₁₇NO₅
• 分子量: 279.293
• InChiKey: XTXWIQLUFDMWBI-UHFFFAOYSA-N

物化性质

• 沸点：
  489.4±45.0 °C(Predicted)
• 密度：
  1.372±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  87.1
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  1-benzyloxycarbonyl-4-hydroxypiperidine-4-carboxylic acid 在 四丁基溴化铵 、 sodium iodide 、 sodium hydroxide 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 14.17h， 生成 C₁₅H₁₈N₂O₄
  参考文献：
  名称：

  一种氧氮杂螺环类化合物的制备方法

  摘要：

  本发明公开了一种氧氮杂螺环类化合物的制备方法，包括以下步骤：以取代的饱和氮杂环烷烃(化合物II)为原料，在碱性条件下水解得化合物III；化合物III与化合物IV(卤代烷基胺)/化合物IV的盐缩合反应生成化合物V；最后化合物V在碱性条件下关环得内酰胺类氧氮杂螺环类化合物I。

  公开号：

  CN111484507B
• 作为产物：
  描述：

  1-benzyl-4-methyl-4-hydroxypiperidine-1,4-dicarboxylate 在 水 、 lithium hydroxide 作用下， 以 乙醇 为溶剂， 反应 18.0h， 以89.3%的产率得到1-benzyloxycarbonyl-4-hydroxypiperidine-4-carboxylic acid
  参考文献：
  名称：

  一种氧氮杂螺环类化合物的制备方法

  摘要：

  本发明公开了一种氧氮杂螺环类化合物的制备方法，包括以下步骤：以取代的饱和氮杂环烷烃(化合物II)为原料，在碱性条件下水解得化合物III；化合物III与化合物IV(卤代烷基胺)/化合物IV的盐缩合反应生成化合物V；最后化合物V在碱性条件下关环得内酰胺类氧氮杂螺环类化合物I。

  公开号：

  CN111484507B

文献信息

• Phosphonic acid derivatives having carboxypeptidase b inhibitory activity
  申请人：Meiji Seika Kaisha Ltd.

  公开号：US06576627B1

  公开（公告）日：2003-06-10

  A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: wherein R1 represents hydrogen atom, an alkyl group, a substituted alkyl group and the like; R2 and R3 represent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group and the like; X represents —CH2—, —O—, or —NH—; A represents the following group (II): [in which R7 and R8 represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group and the like; R9 and R10 represents hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group and the like] and the like; and E represents hydrogen atom and the like, which has inhibitory activity against carboxypeptidase B and is useful for therapeutic and/or preventive treatment of a thrombotic disease.

  以下是通用公式（I）及其药理学上可接受的盐所代表的化合物： 其中R1代表氢原子、烷基、取代烷基等；R2和R3代表氢原子、烷基、取代烷基、烷氧基等；X代表—CH2—、—O—或—NH—；A代表以下的基团（II）： 【其中R7和R8代表氢原子、烷基、酰基、烷氧羰基等；R9和R10代表氢原子、卤素原子、羟基、苯基、烷基等】等；E代表氢原子等，具有对羧肽酶B的抑制活性，并且对治疗和/或预防血栓性疾病有用。
• Gold(I)-Catalyzed Intramolecular Hydroamination and Hydroalkoxylation of Alkynes: Access to Original Heterospirocycles
  作者：Kossi Efouako Soklou、Hamid Marzag、Jean-Philippe Bouillon、Mathieu Marchivie、Sylvain Routier、Karen Plé

  DOI：10.1021/acs.orglett.0c02070

  日期：2020.8.7

  to excellent yields. We have prepared a library of protected amines and tertiary alcohols that give, upon cyclization with alkynes, a representative set of heterospirocycles and illustrate reaction compatibility with diverse functional groups. A change in catalytic activity is possible by modifying the solvent, and two original tricyclic spirocycles were synthesized in a tandem reaction.

  我们在这里报告了一个简单而健壮的金催化环化反应，使N-和O-螺环的产率高至极佳。我们已经准备了一个受保护的胺和叔醇文库，该文库在与炔烃环化后可提供一组代表性的杂环化合物，并说明了与各种官能团的反应相容性。通过改性溶剂可以改变催化活性，并且在串联反应中合成了两个原始的三环螺环。
• Phosphonic acid derivative having inhibitory activity against carboxypeptidase B
  申请人：Meiji Seika Kaisha Ltd.

  公开号：US20030119787A1

  公开（公告）日：2003-06-26

  A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: 1 wherein R 1 represents hydrogen atom, an alkyl group, a substituted alkyl group and the like; R 2 and R 3 represent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group and the like; X represents —CH 2 —, —O—, or —NH—; A represents the following group (II): 2 [in which R 7 and R 8 represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group and the like; R 9 and R 10 represents hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group and the like] and the like; and E represents hydrogen atom and the like, which has inhibitory activity against carboxypeptidase B and is useful for therapeutic and/or preventive treatment of a thrombotic disease.

  以下是通用式（I）及其药学上可接受的盐所代表的化合物：其中R1代表氢原子、烷基、取代烷基等；R2和R3代表氢原子、烷基、取代烷基、烷氧基等；X代表—CH2—、—O—或—NH—；A代表以下基团（II）：其中R7和R8代表氢原子、烷基、酰基、烷氧羰基等；R9和R10代表氢原子、卤素原子、羟基、苯基、烷基等；E代表氢原子等，具有对羧肽酶B的抑制活性，可用于治疗和/或预防血栓性疾病。
• PHOSPHONIC ACID DERIVATIVES HAVING CARBOXYPEPTIDASE B INHIBITORY ACTIVITY
  申请人：Meiji Seika Kaisha, Ltd.

  公开号：EP1152004A1

  公开（公告）日：2001-11-07

  A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: wherein R1 represents hydrogen atom, an alkyl group, a substituted alkyl group and the like; R2 and R3 represent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group and the like; X represents -CH2-, -O-, or -NH-; A represents the following group (II): [in which R7 and R8 represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group and the like; R9 and R10 represents hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group and the like] and the like; and E represents hydrogen atom and the like, which has inhibitory activity against carboxypeptidase B and is useful for therapeutic and/or preventive treatment of a thrombotic disease.

  由以下通式（I）代表的化合物及其药理学上可接受的盐： 其中 R1 代表氢原子、烷基、取代的烷基等；R2 和 R3 代表氢原子、烷基、取代的烷基、烷氧基等；X 代表 -CH2-、-O- 或 -NH-；A 代表以下基团 (II)： [其中 R7 和 R8 代表氢原子、烷基、酰基、烷氧基羰基等；R9 和 R10 代表氢原子、卤素原子、羟基、苯基、烷基等]等；E 代表氢原子等，对羧肽酶 B 具有抑制活性，可用于血栓性疾病的治疗和/或预防。
• Phosphonic acid derivatives having carboxypeptidase B inhibitory action
  申请人：Meiji Seika Kaisha, Ltd.

  公开号：EP1152004B1

  公开（公告）日：2003-05-07