(R)-tert-butyl 3-((R)-1-(3-chlorophenyl)-1-hydroxybutyl)piperidine-1-carboxylate | 1240129-20-7

• 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: (R)-tert-butyl 3-((R)-1-(3-chlorophenyl)-1-hydroxybutyl)piperidine-1-carboxylate
• 英文别名: tert-butyl (3R)-3-[(1R)-1-(3-chlorophenyl)-1-hydroxybutyl]piperidine-1-carboxylate
• CAS: 1240129-20-7
• 化学式: C₂₀H₃₀ClNO₃
• 分子量: 367.916
• InChiKey: MCRFAFRRSKQOHB-UZLBHIALSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  25
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.65
• 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：

  (R)-tert-butyl 3-((R)-1-(3-chlorophenyl)-1-hydroxybutyl)piperidine-1-carboxylate 、 （2-溴乙氧基）-特丁基二甲基硅烷 在 sodium hydride 作用下， 以 四氢呋喃 为溶剂， 反应 2.0h， 以10%的产率得到(R)-tert-butyl 3-((R)-1-(2-(tert-butyldimethylsilyloxy)ethoxy)-1-(3-chlorophenyl)butyl)piperidine-1-carboxylate
  参考文献：
  名称：

  WO2007/70201

  摘要：

  公开号：

文献信息

• [EN] PROCESS FOR PRODUCING 2-(PHENYL METHYL THIO)-3-PYRIDINE CARBOXYLIC ACID<br/>[FR] PROCEDE POUR PRODUIRE DE L'ACIDE 2-(PHENYL METHYL THIO)-3-PYRIDINE CARBOXYLIQUE
  申请人：JUBILANT ORGANOSYS LTD

  公开号：WO2005097748A1

  公开（公告）日：2005-10-20

  The invention discloses an improved process for producing an intermediate to produce large quantity of 2-(Phenyl methyl thio)-3-pyridine carboxylic acid. The process comprises reacting 2-chloro-3-cyanopyridine with benzyl mercaptan in presence of a base and an aprotic solvent. The resulting intermediate 2-(phenyl methyl thio)-3-cyanopyridine is hydrolyzed in presence of a base in an autoclave and isolated under acidic condition to get the desired product.

  该发明揭示了一种改进的生产过程，用于生产大量2-(苯甲硫基)-3-吡啶羧酸的中间体。该过程包括在碱和无极性溶剂存在下，将2-氯-3-氰基吡啶与苄硫醇反应。得到的中间体2-(苯甲硫基)-3-氰基吡啶在高压釜中在碱的存在下水解，并在酸性条件下分离，从而得到所需的产物。
• Process For Producing 2-(Phenyl Methyl Thio)-3-Pyridine Carboxylic Acid
  申请人：Singh Shailendra Kumar

  公开号：US20080139817A1

  公开（公告）日：2008-06-12

  The invention discloses an improved process for producing an intermediate to produce large quantity of 2-(Phenyl methyl thio)-3-pyridine carboxylic acid. The process comprises reacting 2-chloro-3-cyanopyridine with benzyl mercaptan in presence of a base and an aprotic solvent. The resulting intermediate 2-(phenyl methyl thio)-3-cyanopyridine is hydrolyzed in presence of a base in an autoclave and isolated under acidic condition to get the desired product.

  本发明公开了一种改进的生产中间体以生产大量2-(苯甲基硫基)-3-吡啶羧酸的方法。该方法包括在碱和无极溶剂的存在下，将2-氯-3-氰基吡啶与苯甲硫醇反应。所得的中间体2-(苯甲基硫基)-3-氰基吡啶在高压釜中在碱的存在下水解，并在酸性条件下分离，以得到所需的产物。
• Aspartic Protease Inhibitors
  申请人：Baldwin John J.

  公开号：US20100048636A1

  公开（公告）日：2010-02-25

  The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.

  本发明涉及天冬氨酸蛋白酶抑制剂。本发明所述的某些天冬氨酸蛋白酶抑制剂可以用以下结构式或其药学上可接受的盐来表示。本发明还涉及包括所述天冬氨酸蛋白酶抑制剂的药物组合物。本发明还涉及在需要拮抗一种或多种天冬氨酸蛋白酶的主体中的方法，以及使用所述天冬氨酸蛋白酶抑制剂治疗天冬氨酸蛋白酶介导的疾病的方法。
• Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors
  申请人：Baldwin John J.

  公开号：US08487108B2

  公开（公告）日：2013-07-16

  The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.

  本发明涉及天冬氨酸蛋白酶抑制剂。本发明的某些天冬氨酸蛋白酶抑制剂可以用以下结构式或其药学上可接受的盐来表示。本发明还涉及包含所述天冬氨酸蛋白酶抑制剂的制药组合物。本发明还涉及在需要拮抗一种或多种天冬氨酸蛋白酶的受体的主体中的方法，以及使用所述天冬氨酸蛋白酶抑制剂治疗天冬氨酸蛋白酶介导的疾病的方法。
• ASPARTIC PROTEASE INHIBITORS
  申请人：Vitae Pharmaceuticals, Inc.

  公开号：EP1966139B1

  公开（公告）日：2011-12-21