N-(3-dimethylaminopropyl)-5-isoquinolinesulfonamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异喹啉及其衍生物
• 英文名称: N-(3-dimethylaminopropyl)-5-isoquinolinesulfonamide
• 英文别名: N-[3-(dimethylamino)propyl]isoquinoline-5-sulfonamide
• 化学式: C₁₄H₁₉N₃O₂S
• 分子量: 293.39
• InChiKey: OMQGGBZLIOJPMN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  20
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  70.7
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  异喹啉-5-磺酰氯 、 N,N-二甲基-1,3-二氨基丙烷 在 三乙胺 作用下， 以 氯仿 为溶剂， 以71%的产率得到N-(3-dimethylaminopropyl)-5-isoquinolinesulfonamide
  参考文献：
  名称：

  Isoquinolinesulfonyl derivatives and process for the preparation thereof

  摘要：

  一种Formula (I)的5-异喹啉磺酰衍生物：其中l为零或一；m和n均为1至9的整数；m+n至少为一个整数；R.sub.1为氢原子，C.sub.1-10烷基，C.sub.5-6环烷基或芳基；或R.sub.2和R.sub.3各自为氢原子，C.sub.1-10烷基，C.sub.5-6环烷基，芳基或芳基烷基；R.sub.2和R.sub.3为C.sub.1-6烷基基团，并直接或通过氧原子连接形成与相邻氮原子共轭的5-至7-成员杂环环；或##STR2##基团为##STR3##基团，其中R.sub.4和R.sub.5各自为氢原子，C.sub.1-10烷基，芳基或芳基烷基，R.sub.6为氢原子，C.sub.1-10烷基，芳基，芳基烷基，苯甲酰基，肉桂基，肉桂酰基，呋喃基或##STR4##基团，其中R.sub.7为C.sub.1-8烷基；以及其药学上可接受的盐；以及其制备方法。该发明的化合物对血管平滑肌具有松弛作用，并可用作血管扩张剂和降压剂。

  公开号：

  US04456757A1

文献信息

• Isoquinolinesulfonyl derivatives
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：US04525589A1

  公开（公告）日：1985-06-25

  A 5-isoquinolinesulfonyl derivative of Formula (I): ##STR1## wherein l is zero or one; m and n each is an integer of one to nine; m+n is an integer of at least one R.sub.1 is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group or an aryl group; or R.sub.2 and R.sub.3 each is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group, an aryl group or an aralkyl group; R.sub.2 and R.sub.3 are C.sub.1-6 alkylene groups and linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring with the adjacent nitrogen atom; or the ##STR2## group is a ##STR3## group wherein R.sub.4 and R.sub.5 each is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group or an aralkyl group and R.sub.6 is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group, an aralkyl group, a benzoyl group, a cinnamyl group, a cinnamoyl group, a furoyl group or a ##STR4## group wherein R.sub.7 is a C.sub.1-8 alkyl group; and the pharmaceutically acceptable salt thereof; and a process for the preparation thereof. The compounds of this invention have a relaxatory action for vascular smooth muscle and are useful as a vasodilator and a hypotensor.

  公式（I）的5-异喹啉磺酰衍生物：##STR1## 其中l为零或一；m和n均为1至9的整数；m+n至少为1的整数；R.sub.1为氢原子，C.sub.1-10烷基，C.sub.5-6环烷基或芳基；或R.sub.2和R.sub.3均为氢原子，C.sub.1-10烷基，C.sub.5-6环烷基，芳基或芳基烷基；R.sub.2和R.sub.3是C.sub.1-6烷基，直接或通过氧原子与相邻的氮原子形成5-至7-成员杂环环；或##STR2##基团是##STR3##基团，其中R.sub.4和R.sub.5均为氢原子，C.sub.1-10烷基，芳基或芳基烷基，R.sub.6为氢原子，C.sub.1-10烷基，芳基，芳基烷基，苯甲酰基，肉桂基，肉桂酰基，呋喃基或##STR4##基团，其中R.sub.7为C.sub.1-8烷基；以及其药学上可接受的盐；以及其制备过程。该发明化合物对血管平滑肌具有松弛作用，可用作扩血管剂和降压剂。
• Isoquinolinesulfonyl derivatives which possess a relaxatory action
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：US04560755A1

  公开（公告）日：1985-12-24

  A 5-isoquinolinesulfonyl derivative of Formula (I): ##STR1## wherein l is zero or one; m and n each is an integer of one to nine; m+n is an integer of at least one; R.sub.1 is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group or an aryl group; or R.sub.2 and R.sub.3 each is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group, an aryl group or an aralkyl group; R.sub.2 and R.sub.3 are C.sub.1-6 alkylene groups and linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring with the adjacent nitrogen atom; or the ##STR2## wherein R.sub.4 and R.sub.5 each is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group or an aralkyl group and R.sub.6 is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group, an aralkyl group, a benzoyl group, a cinnamyl group, a cinnamoyl group, a furoyl group or a ##STR3## wherein R.sub.7 is a C.sub.1-8 alkyl group; and the pharmaceutically acceptable salt thereof; and a process for the preparation thereof. The compounds of this invention have a relaxatory action for vascular smooth muscle and are useful as a vasodilator and a hypotensor.

  公式（I）的5-异喹啉磺酰衍生物：##STR1## 其中l为零或一；m和n各为1到9的整数；m+n至少为1的整数；R1为氢原子，C1-10烷基，C5-6环烷基或芳基；或R2和R3各为氢原子，C1-10烷基，C5-6环烷基，芳基或芳基烷基；R2和R3为C1-6烷基，直接或通过氧原子与相邻的氮原子连接，形成5-至7-成员的杂环环与；或##STR2## 其中R4和R5各为氢原子，C1-10烷基，芳基或芳基烷基，R6为氢原子，C1-10烷基，芳基，芳基烷基，苯甲酰基，肉桂基，肉桂酰基，呋喃基或##STR3## 其中R7为C1-8烷基；以及其药学上可接受的盐；以及其制备过程。本发明的化合物具有血管平滑肌松弛作用，可用作血管扩张剂和降压剂。
• US4456757A
  申请人：——

  公开号：US4456757A

  公开（公告）日：1984-06-26
• US4525589A
  申请人：——

  公开号：US4525589A

  公开（公告）日：1985-06-25
• US4560755A
  申请人：——

  公开号：US4560755A

  公开（公告）日：1985-12-24