tert-butyl 4-((methylsulfonyloxy)(pyridin-2-yl)methyl)piperidine-1-carboxylate | 333986-06-4

• 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-((methylsulfonyloxy)(pyridin-2-yl)methyl)piperidine-1-carboxylate
• 英文别名: 1-tert-Butoxycarbonyl-4-[(methylsulfonyloxy)(pyridin-2-yl)methyl]piperidine；1-tert-Butoxycarbonyl-4-[(methylsulfonyloxy)(2-pyridyl)methyl]piperidine；tert-butyl 4-[methylsulfonyloxy(pyridin-2-yl)methyl]piperidine-1-carboxylate
• CAS: 333986-06-4
• 化学式: C₁₇H₂₆N₂O₅S
• 分子量: 370.47
• InChiKey: NHCFKOFEODOPHH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 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：
  94.2
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  tert-butyl 4-((methylsulfonyloxy)(pyridin-2-yl)methyl)piperidine-1-carboxylate 在 palladium-carbon 作用下， 以 甲醇 为溶剂， 以92%的产率得到tert-butyl 4-(pyridin-2-ylmethyl)piperidine-1-carboxylate
  参考文献：
  名称：

  Cyclic amine compounds as CCR5 antagonists

  摘要：

  式（I）的化合物（其中R1是氢原子，可能被取代的碳氢基团，可能被取代的非芳香杂环基团，R2是可能被取代的碳氢基团，可能被取代的非芳香杂环基团，或R1和R2可以彼此结合与A一起形成可能被取代的杂环基团；A是N或N+—R5.Y−（R5是碳氢基团；Y−是一个对离子）；R3是可能被取代的环烃基团或可能被取代的杂环基团；n为0或1；R4是氢原子，可能被取代的碳氢基团，可能被取代的杂环基团，可能被取代的烷氧基团，可能被取代的芳基氧基团，或可能被取代的氨基团；E是可能被除氧以外的基团取代的二价脂肪族碳氢基团；G1是键，CO或SO2；G2是CO，SO2，NHCO，CONH或OCO；J是亚甲基或氮原子；Q和R中的每一个是键或可能被取代的二价C1-3脂肪族碳氢基团；条件是当G2为OCO时J为亚甲基，当另一个为键时Q和R中的一个不是键，当G1为键时Q和R中的每一个都不被氧基取代）或其盐具有强大的CCR5拮抗活性，并可优势用于治疗或预防人类体内各种HIV引起的传染病（例如艾滋病）。

  公开号：

  US06562978B1
• 作为产物：
  描述：

  4-(羟基(吡啶-2-基)甲基)哌啶-1-羧酸叔丁酯 、 甲基磺酰氯 在 三乙胺 作用下， 反应 18.0h， 以97.7%的产率得到tert-butyl 4-((methylsulfonyloxy)(pyridin-2-yl)methyl)piperidine-1-carboxylate
  参考文献：
  名称：

  WO2007/53345

  摘要：

  公开号：

文献信息

• 2-AMINOPYRIDINE ANALOGS AS GLUCOKINASE ACTIVATORS
  申请人：Aicher Thomas D.

  公开号：US20090156603A1

  公开（公告）日：2009-06-18

  Provided are compounds of formula I that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes meilitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

  提供了化学式I的化合物，这些化合物在治疗和/或预防由胰岛素活性不足引起的疾病中非常有用，例如糖尿病。还提供了治疗或预防由胰岛素活性不足或可以通过激活胰岛素来治疗的疾病和疾患的方法。
• [EN] CYCLIC AMINE COMPOUNDS AS CCR5 ANTAGONISTS<br/>[FR] COMPOSES D'AMINE CYCLIQUE UTILISES COMME ANTAGONISTES DE CCR5
  申请人：TAKEDA CHEMICAL INDUSTRIES LTD

  公开号：WO2001025200A1

  公开（公告）日：2001-04-12

  A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R?1 and R2¿ may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N?+-R5 •Y-(R5¿ is a hydrocarbon group; Y- is a counter anion); R3 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; n is 0 or 1; R4 is a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, an alkoxy group which may be substituted, an aryloxy group which may be substituted, or an amino group which may be substituted, E is a divalent aliphatic hydrocarbon group which may be substituted by group(s) other than oxo; G1 is a bond, CO or SO¿2; G?2 is CO, SO¿2?, NHCO, CONH or OCO; J is methine or a nitrogen atom; and each of Q and R is a bond or a divalent C1-3 aliphatic hydrocarbon which may be substituted; provided that J is methine when G2 is OCO, that one of Q and R is not a bond when the other is a bond and that each of Q and R is not substituted by oxo group(s) when G?1¿ is a bond) or a salt thereof has a potent CCR5 antagonistic activity and can be advantageously used for the treatment or prevention of infectious disease of various HIV in human (e.g. AIDS).

  化合物式为（I）（其中R1是氢原子，可被取代的碳氢基团，可被取代的非芳香杂环基团，R2是可被取代的碳氢基团，可被取代的非芳香杂环基团，或R1和R2可以与A一起结合形成可被取代的杂环基团；A是N或N+ -R5 • Y-（R5是碳氢基团；Y-是反离子）；R3是可被取代的环烃基团或可被取代的杂环基团；n为0或1；R4是氢原子，可被取代的碳氢基团，可被取代的杂环基团，可被取代的烷氧基，可被取代的芳氧基，或可被取代的氨基，E是可被除氧基以外的基取代的二价脂肪烃基团；G1是键，CO或SO2；G2是CO，SO2，NHCO，CONH或OCO；J是甲基或氮原子；Q和R中的每一个都是一个键或一个可被取代的二价C1-3脂肪基团；前提是当G2是OCO时，J是甲基，当另一个是键时，其中一个不是键，当G1是键时，Q和R中的每一个都没有被氧基团取代）或其盐具有强效的CCR5拮抗活性，并可用于人类各种HIV感染疾病（例如艾滋病）的治疗或预防。
• GLUCOKINASE ACTIVATORS
  申请人：Aicher Thomas D.

  公开号：US20100056530A1

  公开（公告）日：2010-03-04

  Provided are compounds of Formula I wherein R 1 , R 2 , Y, Z and G are as defined herein, that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

  提供了式I化合物，其中R1、R2、Y、Z和G的定义如本文所述，这些化合物对于治疗和/或预防由胰岛素敏感性激酶活性不足引起的疾病（如糖尿病）是有用的。还提供了治疗或预防由胰岛素敏感性激酶活性不足或可以通过激活胰岛素敏感性激酶来治疗的疾病和疾病的方法。
• 2-aminopyridine analogs as glucokinase activators
  申请人：Array Biopharma, Inc.

  公开号：US08022223B2

  公开（公告）日：2011-09-20

  Provided are compounds of formula I that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes meilitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

  提供了I式化合物，可用于治疗和/或预防由葡萄糖激酶活性不足引起的疾病，例如糖尿病。还提供了治疗或预防葡萄糖激酶活性不足或可以通过激活葡萄糖激酶治疗的疾病和紊乱的方法。
• Glucokinase activators
  申请人：Aicher Thomas D.

  公开号：US08933077B2

  公开（公告）日：2015-01-13

  Provided are compounds of Formula I wherein R1, R2, Y, Z and G are as defined herein, that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

  提供了I式化合物，其中R1，R2，Y，Z和G的定义如本文所述，这些化合物在治疗和/或预防由葡萄糖激酶活性不足介导的疾病，如糖尿病方面具有用途。还提供了用于治疗或预防由葡萄糖激酶活性不足或可以通过激活葡萄糖激酶治疗的疾病和障碍的方法。