(6-乙烯基-3-吡啶基)甲醇 | 432554-92-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: (6-乙烯基-3-吡啶基)甲醇
• 英文名称: 2-vinyl-5-hydroxymethylpyridine
• 英文别名: (6-vinylpyridin-3-yl)methanol；(6-Ethenylpyridin-3-yl)methanol
• CAS: 432554-92-2
• 化学式: C₈H₉NO
• 分子量: 135.166
• InChiKey: NPXRTHTXQJNMHF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  33.1
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (6-乙烯基-3-吡啶基)甲醇 、 2,3,4,6-四乙酰氧基-alpha-D-吡喃葡萄糖溴化物 在 silver trifluoromethanesulfonate 作用下， 以 二氯甲烷 为溶剂， 以73%的产率得到
  参考文献：
  名称：

  Functionalizing reagents and their uses

  摘要：

  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。

  公开号：

  US09212148B2
• 作为产物：
  描述：

  三丁基乙烯基锡 、 6-溴-3-羟甲基吡啶 在 四(三苯基膦)钯 作用下， 以 甲苯 为溶剂， 生成 (6-乙烯基-3-吡啶基)甲醇
  参考文献：
  名称：

  Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCθ inhibitors

  摘要：

  Analog 8, a 3-pyridinecarbonitrile with an (E)-2-{6-[(4-methylpiperazin-1-yl) methyl]pyridin-2-yl} vinyl group at C-5, had an IC(50) value of 1.1 nM for the inhibition of PKC theta and potently blocked the production of IL-2 in both stimulated murine T cells (IC(50) = 34 nM) and human whole blood (IC(50) = 500 nM). (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.01.119

文献信息

• Isoxazolines as Therapeutic Agents
  申请人：Calderwood David J.

  公开号：US20130023526A1

  公开（公告）日：2013-01-24

  The present invention provides compound of Formula (I) biologically active metabolites, pro-drugs, isomers, stereoisomers, solvates, hydrates and pharmaceutically acceptable salts thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological conditions.

  本发明提供了化合物Formula（I）的生物活性代谢产物、前药、异构体、立体异构体、溶剂合物、水合物和其药学上可接受的盐，其中变量在此处定义。本发明的化合物对治疗免疫状况有用。
• Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition
  申请人：——

  公开号：US20040043982A1

  公开（公告）日：2004-03-04

  The present invention provides a compound of formula (I) wherein A is an optionally substituted C1-4alkylidene group or a bond, R20 and R21 are hydrogen, alkyl groups or heterocyclic groups, R1 and R2 are small substituents or hydrogen, L is O, S or substituted N, X is a 5-or 6-membered heteroaromatic ring, Y is C1-4alkylidene and Z is a 5- or 6-membered heteroaromatic ring; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; its use in making medicaments for treating neurodegenerative disease and methods of using it to enhance cognition.

  本发明提供了化合物(I)的结构式，其中A是可选取代的C1-4烷基亚甲基或键合，R20和R21是氢、烷基或杂环基，R1和R2是小的取代基或氢，L是O、S或取代的N，X是5-或6-成员杂芳基环，Y是C1-4烷基亚甲基，Z是5-或6-成员杂芳基环；或其药学上可接受的盐；包括它的制药组合物；其在治疗中的用途；其用于制造治疗神经退行性疾病的药物和使用它以增强认知能力的方法。
• 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。
• Isoxazolines as therapeutic agents
  申请人：Calderwood David J.

  公开号：US09029409B2

  公开（公告）日：2015-05-12

  The present invention provides compound of Formula (I) biologically active metabolites, pro-drugs, isomers, stereoisomers, solvates, hydrates and pharmaceutically acceptable salts thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological conditions.

  本发明提供了公式(I)的化合物，其包括生物活性代谢物、前药、异构体、立体异构体、溶剂化物、水合物和其药学上可接受的盐，其中变量在此定义。本发明的化合物用于治疗免疫疾病。