7a-chloromethyl-hexahydro-pyrrolizin | 149948-04-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯里西啶类
• 英文名称: 7a-chloromethyl-hexahydro-pyrrolizin
• 英文别名: 7a-Chlormethyl-hexahydro-pyrrolizin；5-chloromethyl-1-azabicyclo[3.3.0]octane；7a-(chloromethyl)-hexahydro-1H-pyrrolizine；8-(chloromethyl)-1,2,3,5,6,7-hexahydropyrrolizine
• CAS: 149948-04-9
• 化学式: C₈H₁₄ClN
• mdl: MFCD10699452
• 分子量: 159.659
• InChiKey: VYIFNDQTQKCAKZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  7a-chloromethyl-hexahydro-pyrrolizin 在 palladium on activated charcoal 、 乙醇 、 丙酮 作用下， 生成 7a-methyl-2,3,5,6,7,7a-hexahydro-1H-pyrrolizine
  参考文献：
  名称：

  Leonard; Shoemaker, Journal of the American Chemical Society, 1949, vol. 71, p. 1761

  摘要：

  DOI：
• 作为产物：
  描述：

  alkaline earth salt of/the/ methylsulfuric acid 在 氯化亚砜 、 氯仿 作用下， 生成 7a-chloromethyl-hexahydro-pyrrolizin
  参考文献：
  名称：

  Leonard; Shoemaker, Journal of the American Chemical Society, 1949, vol. 71, p. 1761

  摘要：

  DOI：

文献信息

• Nootropic agents, compositions of, and method of use thereof
  申请人：Sanawa Kagaku Kenkyusho Company, Ltd.

  公开号：US05434165A1

  公开（公告）日：1995-07-18

  An aromatic amino-substituted compound represented by formula: ##STR1## wherein A represents CH, N, or N.fwdarw.O; R.sub.1 represents a nitro group or an amino group; R.sub.2 represents a hydrogen atom, a lower alkyl group, or an acyl group; and R.sub.3 represents a group: ##STR2## wherein m represents 0 or 1; n represents an integer of from 0 to 3; R.sub.4 and R.sub.5 each represents a hydrogen atom or a lower alkyl group; R.sub.6 and R.sub.7 each represents a hydrogen atom or a straight chain or branched lower alkyl group; R.sub.4 and R.sub.6 may be joined together to form an alkylene chain forming a heterocyclic ring; R.sub.5 and R.sub.7 may be joined together to form an alkylene chain forming a heterocyclic ring and R.sub.6 and R.sub.7 may be joined together to form an alkylene chain forming a heterocyclic ring, or a pharmaceutically acceptable salt thereof, a process for producing the same, and a method for preventing or treating brain disfunction such as senile dementia or Alzheimer's disease by administering a nootropic agent containing the same as an active ingredient are disclosed.

  一种芳香族氨基取代化合物，其化学式表示为：##STR1## 其中A代表CH、N或N.fwdarw.O；R.sub.1代表硝基基团或氨基团；R.sub.2代表氢原子、较低的烷基基团或酰基团；R.sub.3代表一个基团：##STR2## 其中m表示0或1；n表示0到3的整数；R.sub.4和R.sub.5分别代表氢原子或较低的烷基基团；R.sub.6和R.sub.7分别代表氢原子或直链或支链较低的烷基基团；R.sub.4和R.sub.6可以结合在一起形成形成杂环环的烷基链；R.sub.5和R.sub.7可以结合在一起形成形成杂环环的烷基链，R.sub.6和R.sub.7可以结合在一起形成形成杂环环的烷基链，或其药学上可接受的盐，公开了一种制备该化合物的方法，以及通过给予含有该化合物作为活性成分的智力药剂来预防或治疗脑功能障碍，如老年性痴呆症或阿尔茨海默病的方法。
• 1-Azabicyclo(3.3.0)octane derivatives and their use
  申请人：SANWA KAGAKU KENKYUSHO CO., LTD.

  公开号：EP0647642A1

  公开（公告）日：1995-04-12

  There is disclosed a compound shown by a formula of    wherein R₁ is a hydrogen atom, alkyl group having 1 - 4 carbon atoms or acyl group having 1 - 4 carbon atoms; R₂ and R₃ are a hydrogen atom, alkyl group having 1 - 4 carbon atoms, phenyl radical, halogen atom, cyano radical, acyl group having 1 - 4 carbon atoms, nitro radical, alkoxy group having 1 or 2 carbon atoms, or substituted or non-substituted amino group, respectively; n is an integer of 1 - 3; and dotted line means a possible ring, and a salt thereof. The compound and salt bind with muscarinic receptor in brain to develop a powerful actuation thereof and thus those can be used as an effective ingredient for preventing and curing senile dementias, and more particularly Alzheimer's disease.

  本发明揭示了一种化合物，其化学式如下：其中，R₁表示氢原子、1-4个碳原子的烷基或1-4个碳原子的酰基基团；R₂和R₃分别表示氢原子、1-4个碳原子的烷基、苯基、卤原子、氰基、1-4个碳原子的酰基、硝基、1或2个碳原子的烷氧基或取代或未取代的氨基基团；n是1-3的整数；虚线表示可能的环，并且其盐。该化合物和盐与大脑中的肌动蛋白受体结合，从而发挥强大的作用，因此可以用作预防和治疗老年痴呆症，特别是阿尔茨海默病的有效成分。
• Compounds and use thereof
  申请人：Sanwa Kagaku Kenkyusho Co., Ltd.

  公开号：US05530138A1

  公开（公告）日：1996-06-25

  There is disclosed a compound shown by a formula of ##STR1## wherein R.sub.1 is a hydrogen atom alkyl group having 1-4 carbon atoms or acyl group having 1-4 carbon atoms: R.sub.2 and R.sub.3 are a hydrogen atom, alkyl group having 1-4 carbon atoms, phenyl radical, halogen atom, cyano radical, acyl group having 1-4 carbon atoms, nitro radical, alkoxy group having 1 or 2 carbon atoms, or substituted or non-substituted amino group, respectively; n is an integer of 1-3; and dotted line means a possible ring, and a salt thereof. The compound and salt bind with muscarinic receptor in brain to develop a powerful actuation thereof and thus those can be used as an effective ingredient for preventing and curing senile dementias, and more particularly Alzheimer's disease.

  本发明披露了一种化合物，其化学式为##STR1##其中，R.sub.1是氢原子烷基，其具有1-4个碳原子或酰基，其具有1-4个碳原子：R.sub.2和R.sub.3分别是氢原子、具有1-4个碳原子的烷基、苯基、卤素原子、氰基、具有1-4个碳原子的酰基、硝基、具有1或2个碳原子的烷氧基或取代或未取代的氨基；n是1-3的整数；虚线表示可能的环，并且包括其盐。该化合物和盐与脑中的肌动蛋白受体结合，以发展其强大的作用，因此可以作为预防和治疗老年痴呆症，特别是阿尔茨海默病的有效成分。
• Pyrrolizidine compounds, methods for their production, and their uses
  申请人：SUNTORY KABUSHIKI KAISHA, also known as SUNTORY LTD.

  公开号：EP0171912A1

  公开（公告）日：1986-02-19

  A novel pyrrolizidine compound of the formula (wherein R1 is an alkyl group of 1 to 4 carbon atoms or a phenyl group; and R2 and R3 are such that at least one of them is an alkyl group of 1 to 4 carbon atoms with the other, if any, being a hydrogen atom) is produced by reacting Δ4(8)-dehydropyrrolizidine with a substituted malonic acid and thus formed 2-substituted-8-pyrrolizidineacetic acid with a substituted aniline. The product is optionally subjected to optical resolution. The pyrrolizidine compound has more potent antiarrhythmic activity than known similar pyrrolizidine compounds.

  一种新型吡咯烷化合物，其式如下 (其中 R1 是 1 至 4 个碳原子的烷基或苯基；R2 和 R3 至少有一个是 1 至 4 个碳原子的烷基，另一个（如有）是氢原子）是通过 Δ4(8)-dehydropyrrolizidine 与取代的丙二酸反应生成的。产物可选择进行光学解析。与已知的类似吡咯烷化合物相比，该吡咯烷化合物具有更强的抗心律失常活性。
• Nootropic agent
  申请人：SANWA KAGAKU KENKYUSHO CO., LTD.

  公开号：EP0543307A2

  公开（公告）日：1993-05-26

  An aromatic amino-substituted compound represented by formula: wherein A represents CH, N, or N→O; R1 represents a nitro group or an amino group; R2 represents a hydrogen atom, a lower alkyl group, or an acyl group; and R3 represents a group: wherein m represents 0 or 1; n represents an integer of from 0 to 3; R4 and R5 each represents a hydrogen atom or a lower alkyl group; R6 and R7 each represents a hydrogen atom or a straight chain or branched lower alkyl group; R4 and R6 may be joined together to form an alkylene chain forming a heterocyclic ring; R5 and R7 may be joined together to form an alkylene chain forming a heterocyclic ring; and R6 and R7 may be joined together to form an alkylene chain forming a heterocyclic ring, or a pharmaceutically acceptable salt thereof, a process for producing the same, and a method for preventing or treating brain disfunction such as senile dementia or Alzheimer's disease by administering a nootropic agent containing the same as an active ingredient are disclosed.

  式所代表的芳香族氨基取代化合物： 其中 A 代表 CH、N 或 N→O；R1 代表硝基或氨基；R2 代表氢原子、低级烷基或酰基；R3 代表一个基团： 其中 m 代表 0 或 1；n 代表 0 至 3 的整数；R4 和 R5 各自代表氢原子或低级烷基；R6 和 R7 各自代表氢原子或直链或支链低级烷基；R4 和 R6 可连接在一起形成形成杂环的亚烷基链；R5 和 R7 可连接在一起形成形成杂环的亚烷基链；以及 R6 和 R7 可连接在一起形成形成杂环的亚烷基链、 或其药学上可接受的盐、生产该物质的工艺，以及通过施用含有该物质作为活性成分的促智剂来预防或治疗大脑功能障碍（如老年痴呆症或阿尔茨海默病）的方法，均已公开。