[5-(1-methyl-pyrrolidin-2-yl)-pyridin-2-yl]-methanol | 67257-85-6

• 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
• 英文名称: [5-(1-methyl-pyrrolidin-2-yl)-pyridin-2-yl]-methanol
• 英文别名: 6-Hydroxymethylnicotin；Hydroxymethylnicotine；[5-(1-methylpyrrolidin-2-yl)pyridin-2-yl]methanol
• CAS: 67257-85-6
• 化学式: C₁₁H₁₆N₂O
• 分子量: 192.261
• InChiKey: HJDCNAJYPGRVAD-UHFFFAOYSA-N

物化性质

• 沸点：
  321.0±42.0 °C(Predicted)
• 密度：
  1.124±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  36.4
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  正丁基锂 、 6-bromonicotine 、 N,N-二甲基甲酰胺 、 硼氢化钠 、 氯化铵 在 氮气 、 methanol-dichloromethane 、 crude residue 、 silica 作用下， 以 hexanes 、 四氢呋喃 、 甲醇 为溶剂， 反应 2.17h， 以to yield the desired hydroxymethylpyridine (100 mg, 26%)的产率得到[5-(1-methyl-pyrrolidin-2-yl)-pyridin-2-yl]-methanol
  参考文献：
  名称：

  Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition

  摘要：

  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。

  公开号：

  US20040043982A1

文献信息

• Hapten-carrier conjugates and uses thereof
  申请人：Bachmann F. Martin

  公开号：US20050281845A1

  公开（公告）日：2005-12-22

  The present invention provides compositions comprising a conjugate of a hapten with a carrier in an ordered and repetitive array, and methods of making such compositions. The conjugates and compositions of the invention may comprise a variety of haptens, including hormones, toxins and drugs, especially drugs of addiction such as nicotine. Compositions and conjugates of the invention are useful for inducing immune responses against haptens, which can use useful in a variety of therapeutic, prophylactic and diagnostic regimens. In certain embodiments, immune responses generated using the conjugates, compositions and methods of the present invention are useful to prevent or treat addiction to drugs of abuse and the resultant diseases associated with drug addiction.

  本发明提供了一种包含半抗原与载体的共轭物的组合物，其具有有序和重复的排列方式，并提供了制备这种组合物的方法。本发明的共轭物和组合物可以包含各种半抗原，包括激素、毒素和药物，特别是成瘾药物如尼古丁。本发明的组合物和共轭物可用于诱导免疫反应，用于各种治疗、预防和诊断方案。在某些实施例中，使用本发明的共轭物、组合物和方法产生的免疫反应可用于预防或治疗药物成瘾及与药物成瘾相关的疾病。
• Hapten-Carrier Conjugates and Uses Thereof
  申请人：BACHMANN Martin F.

  公开号：US20130142821A1

  公开（公告）日：2013-06-06

  The present invention provides compositions comprising a conjugate of a hapten with a carrier in an ordered and repetitive array, and methods of making such compositions. The conjugates and compositions of the invention may comprise a variety of haptens, including hormones, toxins and drugs, especially drugs of addiction such as nicotine. Compositions and conjugates of the invention are useful for inducing immune responses against haptens, which can use useful in a variety of therapeutic, prophylactic and diagnostic regimens. In certain embodiments, immune responses generated using the conjugates, compositions and methods of the present invention are useful to prevent or treat addiction to drugs of abuse and the resultant diseases associated with drug addiction.

  本发明提供了一种由载体和半抗原共价结合的有序和重复阵列的组合物及其制备方法。该发明的共价结合物和组合物可以包含多种半抗原，包括激素、毒素和药物，特别是成瘾药物如尼古丁。本发明的组合物和共价结合物可用于诱导对半抗原的免疫反应，这对于各种治疗、预防和诊断方案都有用。在某些实施例中，使用本发明的共价结合物、组合物和方法产生的免疫反应可用于预防或治疗药物成瘾及与药物成瘾相关的疾病。
• Nicotine-carrier vaccine formulation
  申请人：Cytos Biotechnology AG

  公开号：EP1854478A1

  公开（公告）日：2007-11-14

  The present invention is in the fields of medicine, public health, vaccine and drug formulation. The invention provides composition formulations comprising a nicotine-carrier conjugate and a stabilizer, wherein said stabilizer comprises a non-reducing disaccharide and a non-ionic surfactant. The composition formulations are stable after a long time of storage at room temperature.

  本发明涉及医药、公共卫生、疫苗和药物制剂领域。本发明提供了由尼古丁-载体共轭物和稳定剂组成的组合物配方，其中所述稳定剂包括非还原性二糖和非离子表面活性剂。该组合物制剂在室温下长时间储存后仍保持稳定。
• Hapten-carrier conjugates comprising virus like particles and uses thereof
  申请人：Cytos Biotechnology AG

  公开号：EP2392345A2

  公开（公告）日：2011-12-07

  The present invention provides compositions comprising a conjugate of a hapten with a carrier in an ordered and repetitive array, and methods of making such compositions. The conjugates and compositions of the invention comprise drugs, especially drugs of addiction such as nicotine. Compositions and conjugates of the invention are useful for inducing immune responses against haptens, which can use useful in a variety of therapeutic, prophylactic and diagnostic regimens. In certain embodiments, immune responses generated using the conjugates, compositions and methods of the present invention are useful to prevent or treat addiction to drugs of abuse and the resultant diseases associated with drug addiction.

  本发明提供了包含以有序和重复阵列形式存在的合体与载体的共轭物的组合物，以及制造这种组合物的方法。本发明的共轭物和组合物包含药物，特别是成瘾药物，如尼古丁。本发明的组合物和共轭物可用于诱导针对合体的免疫反应，这可用于各种治疗、预防和诊断方案。在某些实施方案中，使用本发明的共轭物、组合物和方法产生的免疫反应可用于预防或治疗对滥用药物的成瘾以及由此导致的与药物成瘾相关的疾病。
• COMPOSITIONS AND COMPOUNDS FOR USE AS A NICOTINE VACCINE EMPLOYING RESPONSE SELECTIVE AGONIST OF AN ANTIGEN-PRESENTING CELL RECEPTOR AS A MOLECULAR ADJUVANT
  申请人：The Board of Regents of the University of Nebraska

  公开号：EP1480672A2

  公开（公告）日：2004-12-01