8-piperidinooctan-1-amine | 154620-13-0

• 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: 8-piperidinooctan-1-amine
• 英文别名: 8-piperidinyloctylamine；8-piperidin-1-yloctan-1-amine
• CAS: 154620-13-0
• 化学式: C₁₃H₂₈N₂
• 分子量: 212.379
• InChiKey: VRUVRIGKTLVDIA-UHFFFAOYSA-N

物化性质

• 沸点：
  301.6±10.0 °C(Predicted)
• 密度：
  0.893±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  15
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  29.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-氯苯并咪唑 、 8-piperidinooctan-1-amine 以 异戊醇 为溶剂， 反应 16.0h， 以79%的产率得到N-(8-piperidin-1-yloctyl)-1H-benzimidazol-2-amine
  参考文献：
  名称：

  Synthesis and biological evaluation of new non-imidazole H3-receptor antagonists of the 2-aminobenzimidazole series

  摘要：

  A novel series of non-imidazole H-3-receptor antagonists was developed, by chemical modification of a potent lead H-3-antagonist composed by an imidazole ring connected through an alkyl spacer to a 2-aminobenzimidazole moiety (e.g., 2-[[3-[4(5)-imidazolyl]propyl]amino]benzimidazole), previously reported by our research group. We investigated whether the removal of the imidazole ring could allow retaining high affinity for the H-3-receptor, thanks to the interactions undertaken by the 2-aminobenzimidazole moiety at the binding site. The imidazole ring of the lead was replaced by a basic piperidine or by a lipophilic p-chlorophenoxy substituent, modulating the spacer length from three to eight methylene groups; moreover, the substituents were moved to the 5(6) position of the benzimidazole nucleus. Within both the 2-alkylaminobenzimidazole series and the 5(6)-alkoxy-2-amino-benzimidazole one, the greatest H-3-receptor affinity was obtained for the piperidine-substituted compounds, while the presence of the p-chlorophenoxy group resulted in a drop in affinity. The optimal chain length was different in the two series. Even if the new compounds did not reach the high receptor affinity shown by the imidazole-containing lead compound, it was possible to get good H-3-antagonist potencies with 2-aminobenzimidazoles having a tertiary amino group at appropriate distance. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2005.09.063
• 作为产物：
  描述：

  1,8-二溴辛烷 在 盐酸 、 potassium iodide 作用下， 以 丙酮 为溶剂， 反应 96.0h， 生成 8-piperidinooctan-1-amine
  参考文献：
  名称：

  与组合抑制组胺N-甲基转移酶活性的新型一类新的非咪唑组胺H（3）受体配体的发展。

  摘要：

  在寻找增强中枢神经系统中组胺能神经传递的新颖方法的同时，开发了一种新型的非咪唑组胺H（3）受体配体，该配体同时对主要组胺代谢酶组胺N-甲基转移酶（HMT）具有较强的抑制活性。新化合物包含氨基喹啉部分，这是HMT抑制活性的重要结构特征，通过不同的间隔基连接到哌啶子基上（对H（3）受体有拮抗作用）。间隔物结构的变化提供了两种不同系列的化合物。一个系列，在基本中心之间只有一个亚烷基间隔基，导致对人组胺H（3）受体具有中等至高亲和力的高效HMT抑制剂。第二系列具有对苯氧丙基间隔基 可以被另一个亚烷基链延长。后一个系列还显示出对HMT的强抑制活性，并且在大多数情况下，H（3）受体的亲和力甚至超过了第一个系列。具有这种双重作用方式的最有效的化合物之一是4-（4-（3-哌啶子基丙氧基）苯氨基）喹啉（34）（hH（3），K（i）= 0.09 nM; HMT，IC（50）= 51 nM）。这类化合物在豚鼠对

  DOI：

  10.1021/jm0110845

文献信息

• Aminoalkylcarbamic esters of eseroline suitable for use as
  申请人：Mediolanum Farmaceutici S.p.A.

  公开号：US05302593A1

  公开（公告）日：1994-04-12

  Aminoalkylcarbamic esters of eseroline suitable for use as cholinesterase activity inhibitors, having general formula (I) ##STR1## where R stands for an amine selected out of the group consisting of ##STR2## and n, R1, R2, R3, and R4 are as defined in the text.

  适用于用作胆碱酯酶活性抑制剂的艾色罗林氨基烷基氨基甲酸酯，具有一般式(I) ##STR1## 其中R代表从组中选择的胺之一##STR2## n、R1、R2、R3和R4如文本中定义。
• Process for preparing aminoalkylcarbamic esters of eseroline
  申请人：Mediolanum Farmaceutici S.p.A.

  公开号：US05424451A1

  公开（公告）日：1995-06-13

  Aminoalkylcarbamic esters of eseroline suitable for use as cholinesterase activity inhibitors, having general formula (I) ##STR1## where R stands for an amine selected out of the group consisting of ##STR2## and n, R1, R2, R3, and R4 are as defined in the text.

  适用于作为胆碱酯酶活性抑制剂的eseroline氨基烷基氨基甲酸酯具有一般式（I）## STR1 ##，其中R代表从## STR2 ##组成的胺中选择的胺，n，R1，R2，R3和R4如文本中所定义。
• MODIFIED BLOCK COPOLYMER, METHOD FOR PRODUCING MODIFIED BLOCK COPOLYMER, AND RESIN COMPOSITION
  申请人：Asahi Kasei Kabushiki Kaisha

  公开号：EP3623398A1

  公开（公告）日：2020-03-18

  A modified block copolymer according to the present invention is a modified block copolymer comprising a polymer block comprising a vinyl aromatic compound as a main constituent (A), a polymer block comprising a conjugate diene compound as a main constituent (B), and an atomic group having NHx (x = 0 to 2) (C). In the modified block copolymer, the polymer block comprising a conjugate diene compound as a main constituent (B) is a hydrogenated product, the atomic group having NHx (x = 0 to 2) (C) is contained in a side chain, and a compound forming the atomic group having NHx (x = 0 to 2) (C) satisfies the following condition: Condition: when the compound forming the atomic group having NHx (x = 0 to 2) (C) is reacted with a maleic anhydride-modified group in a maleic anhydride-modified block copolymer, a MFR value at 230°C under a load of 2.16 kg of the modified block copolymer after the reaction is 0.1 times or more a MFR value at 230°C under a load of 2.16 kg of the maleic anhydride-modified block copolymer before the reaction.

  根据本发明，改性嵌段共聚物是一种改性嵌段共聚物，包括以乙烯基芳香族化合物为主要成分的聚合物嵌段（A）、以共轭二烯化合物为主要成分的聚合物嵌段（B）和具有 NHx（x = 0 至 2）的原子团（C）。在改性嵌段聚合物中，由共轭二烯化合物作为主要成分（B）的聚合物嵌段是氢化产物，具有 NHx（x = 0 至 2）（C）的原子团包含在侧链中，形成具有 NHx（x = 0 至 2）（C）的原子团的化合物满足以下条件： 条件：当形成具有 NHx（x = 0 至 2）(C)的原子团的化合物与马来酸酐改性嵌段共聚物中的马来酸酐改性基团反应时，反应后在 230℃、负载 2.16 千克改性嵌段共聚物时的 MFR 值是反应前在 230℃、负载 2.16 千克马来酸酐改性嵌段共聚物时的 MFR 值的 0.1 倍或以上。
• Modified block copolymer, method for producing modified block copolymer, and resin composition
  申请人：Asahi Kasei Kabushiki Kaisha

  公开号：US11124593B2

  公开（公告）日：2021-09-21

  A modified block copolymer according to the present invention is a modified block copolymer comprising a polymer block comprising a vinyl aromatic compound as a main constituent (A), a polymer block comprising a conjugate diene compound as a main constituent (B), and an atomic group having NHx (x=0 to 2) (C). In the modified block copolymer, the polymer block comprising a conjugate diene compound as a main constituent (B) is a hydrogenated product, the atomic group having NHx (x=0 to 2) (C) is contained in a side chain, and a compound forming the atomic group having NHx (x=0 to 2) (C).

  根据本发明，改性嵌段共聚物是一种改性嵌段共聚物，包括以乙烯基芳香族化合物为主要成分的聚合物嵌段（A）、以共轭二烯化合物为主要成分的聚合物嵌段（B）和具有 NHx（x=0 至 2）的原子团（C）。在改性嵌段共聚物中，由共轭二烯化合物作为主要成分（B）的聚合物嵌段是氢化产物，具有 NHx（x=0 至 2）（C）的原子团包含在侧链中，以及形成具有 NHx（x=0 至 2）（C）的原子团的化合物。
• Aminoalkylcarbamic esters of eseroline suitable for use as cholinesterase acitivity inhibitors and relative preparation process
  申请人：MEDIOLANUM FARMACEUTICI S.P.A.

  公开号：EP0575954B1

  公开（公告）日：1998-09-02