(4-bromopyridin-2-yl)methyl 4-methylbenzenesulfonate

• 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: (4-bromopyridin-2-yl)methyl 4-methylbenzenesulfonate
• 英文别名: (4-Bromopyridin-2-yl)methyl 4-methylbenzenesulfonate
• 化学式: C₁₃H₁₂BrNO₃S
• 分子量: 342.213
• InChiKey: IXYBAIWIFYSJHU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  64.6
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (4-bromopyridin-2-yl)methyl 4-methylbenzenesulfonate 在 三氯氧磷 作用下， 生成 7-bromoimidazo[1,5-a]pyridine-1-carbaldehyde
  参考文献：
  名称：

  INHIBITORS OF PLASMA KALLIKREIN AND USES THEREOF

  摘要：

  本发明提供了作为血浆激肽酶抑制剂并具有相同理想特性的化合物和组合物。

  公开号：

  US20190284182A1
• 作为产物：
  描述：

  2-羟甲基-4-溴吡啶 、 对甲苯磺酰氯 生成 (4-bromopyridin-2-yl)methyl 4-methylbenzenesulfonate
  参考文献：
  名称：

  INHIBITORS OF PLASMA KALLIKREIN AND USES THEREOF

  摘要：

  本发明提供了作为血浆激肽酶抑制剂并具有相同理想特性的化合物和组合物。

  公开号：

  US20190284182A1

文献信息

• Functionalizing reagents and their uses
  申请人：Glythera Limited

  公开号：US09212148B2

  公开（公告）日：2015-12-15

  Reagents and methods for functionalizing polypeptides with moieties (alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalizing reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalizing reagent is covalently linked to a poly(alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly(alkylene glycol) molecule and/or the glycan group.

  揭示了用于将多肽功能化为基于功能化试剂的醚基（烷基乙二醇）分子和糖基的方法和试剂，该功能化试剂包括具有乙烯基取代基的含氮杂环芳香环，能够与多肽中天然存在的一个或多个巯基发生反应，或者通过引入巯基（例如通过利用一个或多个半胱氨酸残基的巯基）进入多肽中。功能化试剂与聚（烷基乙二醇）分子（如聚乙二醇（PEG）分子）或糖基共价连接，使得多肽中乙烯基和巯基之间的反应共价连接多肽与聚（烷基乙二醇）分子和/或糖基。
• FUNCTIONALISING REAGENTS AND THEIR USES
  申请人：Watts Andrew Graham

  公开号：US20120101254A1

  公开（公告）日：2012-04-26

  Reagents and methods for functionalising polypeptides with moieties poly (alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalising reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalising reagent is covalently linked to a poly (alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly (alkylene glycol) molecule and/or the glycan group.

  本发明揭示了用于将多元(烷基乙二醇)分子和糖基与多肽进行官能化的试剂和方法，其基于一种官能化试剂，其包括具有乙烯基取代基的含氮杂环芳香环，其能够与自然存在或已经引入多肽中的一个或多个巯基反应，例如通过使用一个或多个半胱氨酸残基的巯基。官能化试剂与多元(烷基乙二醇)分子（例如聚乙二醇(PEG)分子）或糖基共价连接，使得多肽中的乙烯基与巯基之间的反应共价连接多肽和多元(烷基乙二醇)分子和/或糖基。
• FUNCTIONALIZING REAGENTS AND THEIR USES
  申请人：Glythera Limited

  公开号：US20140364586A1

  公开（公告）日：2014-12-11

  Reagents and methods for functionalizing polypeptides with moieties (alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalizing reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalizing reagent is covalently linked to a poly(alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly(alkylene glycol) molecule and/or the glycan group.

  本文披露了一种功能化试剂和方法，用于将（烷基二醇）分子和糖基与多肽功能化。该方法基于一种功能化试剂，该试剂包含一个含氮杂环芳香环，具有一个乙烯基取代基，能够与多肽中天然存在或已引入的一个或多个巯基反应，例如使用一个或多个半胱氨酸残基的巯基。功能化试剂与多（烷基二醇）分子（例如聚乙二醇（PEG）分子）或糖基共价连接，因此，多肽中乙烯基和巯基之间的反应将多肽共价连接到多（烷基二醇）分子和/或糖基上。
• Thiol-functionalising reagents and their uses
  申请人：Glythera Limited

  公开号：EP2886132A1

  公开（公告）日：2015-06-24

  Reagents and methods for functionalising polypeptides with moieties poly(alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalising reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalising reagent is covalently linked to a poly(alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly(alkylene glycol) molecule and/or the glycan group.

  本发明公开了用聚(烷二醇)分子和聚糖基团使多肽功能化的试剂和方法，这些试剂和方法基于一种功能化试剂，该试剂包括一个含氮杂环芳香环，该芳香环具有乙烯基取代基，能够与多肽中天然存在或引入的一个或多个硫醇基反应，例如通过使用一个或多个半胱氨酸残基的硫醇基。官能化试剂与聚(烷二醇)分子（如聚乙二醇（PEG）分子）或聚糖基团共价连接，使乙烯基与多肽中的硫醇基团反应，将多肽与聚(烷二醇)分子和/或聚糖基团共价连接。
• Inhibitors of plasma kallikrein and uses thereof
  申请人：Shire Human Genetic Therapies, Inc.

  公开号：US10730874B2

  公开（公告）日：2020-08-04

  The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.

  本发明提供了可用作血浆钙激酶抑制剂并表现出理想特性的化合物及其组合物。