1-(3-morpholinopropyl)-3-aminoindazole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 英文名称: 1-(3-morpholinopropyl)-3-aminoindazole
• 英文别名: 1-(3-morpholin-4-ylpropyl)indazol-3-amine
• 化学式: C₁₄H₂₀N₄O
• 分子量: 260.339
• InChiKey: ZFQJGHOJTSLMIH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  56.3
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  N,N-二甲基甲酰胺 、 1-(3-morpholinopropyl)-3-aminoindazole 、 3-溴-N,N-二乙基丙氨氢溴酸盐 、 potassium carbonate 在 乙醚 、 盐酸 、 氯仿 、 Sodium sulfate-III 作用下， 以 氯仿 、 水 为溶剂， 反应 12.0h， 以to give 3.50 g of 1-(3-morpholinopropyl)-3-(3-diethylaminopropylamino)indazole having the following analytical values in a yield of 58 %的产率得到1-(3-morpholinopropyl)-3-(3-diethylaminopropylamino)indazole
  参考文献：
  名称：

  Aminoindazole derivatives

  摘要：

  化合物的式子（I）：##STR1## 其中W.sub.1和W.sub.2各自独立地是氢原子或##STR2##基团，其中Y是n-C.sub.1-6烷基或具有C.sub.1-6烷基取代基的n-C.sub.1-6烷基；R.sub.1和R.sub.2各自独立地是氢原子或C.sub.1-6烷基，并且##STR3##在##STR4##基团中可以形成选择自吗啡啶，吡咯烷，哌啶，同哌啶和哌嗪基团的饱和杂环环，除了吗啡啶基团的饱和杂环环可以具有至少一个C.sub.1-4烷基，羟基或卤素原子作为取代基；Z.sub.1是氢原子，氯原子，溴原子，碘原子，羟基，氨基，C.sub.1-3烷基或甲氧基；Z.sub.2是氢原子或氨基；当W.sub.1和W.sub.2都是氢原子时，Z.sub.1是羟基或碘原子，Z.sub.2是氢原子，或者Z.sub.1和Z.sub.2都是氨基；当Z.sub.1和Z.sub.2都是氢原子时，W.sub.1或W.sub.2中的##STR5##基团是吗啡啶基团；当Z.sub.1是氯原子，羟基，碘原子，甲基或甲氧基时，Z.sub.2是氢原子；当Z.sub.1是氨基时，Z.sub.2是氢原子或氨基；当Z.sub.1是甲基，甲氧基或氨基时，Z.sub.1在5位；当Z.sub.1是碘原子时，Z.sub.1在5-或7-位置；当Z.sub.1和Z.sub.2都是氨基时，Z.sub.1和Z.sub.2在5-和7-位置；以及其生理上可接受的酸加成盐，这些化合物具有药用价值，例如：用于治疗炎症。

  公开号：

  US04533731A1
• 作为产物：
  描述：

  3-氨基吲唑 、 3-氨基-5-氯-1H-吲唑 生成 1-(3-morpholinopropyl)-3-aminoindazole
  参考文献：
  名称：

  Aminoindazole derivatives

  摘要：

  式(I)的化合物：其中W.sub.1和W.sub.2各自独立地是氢原子或##STR2##基团，其中Y是n-C.sub.1-6烷基烯基或具有C.sub.1-6烷基基团取代物的n-C.sub.1-6烷基烯基；R.sub.1和R.sub.2各自独立地是氢原子或C.sub.1-6烷基基团，以及##STR3##在##STR4##基团中的基团可能形成从吗啡啉，吡咯啉，哌啶，环己哌啶和哌嗪基团中选择的饱和杂环环；除了吗啡啉基团之外的饱和杂环环可能具有至少一个C.sub.1-4烷基基团，羟基基团或卤原子作为取代物；Z.sub.1是氢原子，氯原子，溴原子，碘原子，羟基，氨基，C.sub.1-3烷基基团或甲氧基基团；Z.sub.2是氢原子或氨基；当W.sub.1和W.sub.2都是氢原子时，Z.sub.1是羟基或碘原子，Z.sub.2是氢原子，或Z.sub.1和Z.sub.2都是氨基；当Z.sub.1和Z.sub.2都是氢原子时，W.sub.1或W.sub.2中的##STR5##基团是吗啡啉基团；当Z.sub.1是氯原子，羟基，碘原子，甲基基团或甲氧基基团时，Z.sub.2是氢原子；当Z.sub.1是氨基时，Z.sub.2是氢原子或氨基；当Z.sub.1是甲基基团，甲氧基基团或氨基时，Z.sub.1在5-位；当Z.sub.1是碘原子时，Z.sub.1在5-位或7-位；当Z.sub.1和Z.sub.2都是氨基时，Z.sub.1和Z.sub.2在5-位和7-位；以及其生理上可接受的酸盐，这些化合物具有药用价值，例如：用于治疗炎症。

  公开号：

  US04533731A1

文献信息

• US4533731A
  申请人：——

  公开号：US4533731A

  公开（公告）日：1985-08-06
• US4751302A
  申请人：——

  公开号：US4751302A

  公开（公告）日：1988-06-14
• Aminoindazole derivatives
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：US04533731A1

  公开（公告）日：1985-08-06

  A compound of the formula (I): ##STR1## wherein W.sub.1 and W.sub.2 each independently is a hydrogen atom or a ##STR2## group wherein Y is a n-C.sub.1-6 alkylene group or a n-C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-6 alkyl group, and ##STR3## group in ##STR4## group may form a saturated heterocyclic ring selected from the group consisting of morpholino, pyrrolidino, piperidino, homopiperidino and piperazino groups, and the saturated heterocyclic ring except the morpholino group may have at least one C.sub.1-4 alkyl group, hydroxyl group or halogen atom as a substituent; Z.sub.1 is a hydrogen atom, a chlorine atom, a bromine atom, an iodine atom, a hydroxyl group, an amino group, a C.sub.1-3 alkyl group or a methoxy group; Z.sub.2 is a hydrogen atom or an amino group; when W.sub.1 and W.sub.2 are both hydrogen atoms, Z.sub.1 is a hydroxyl group or an iodine atom and Z.sub.2 is hydrogen atom, or Z.sub.1 and Z.sub.2 are both amino groups; when Z.sub.1 and Z.sub.2 are both hydrogen atoms, the ##STR5## group in either W.sub.1 or W.sub.2 is a morpholino group; when Z.sub.1 is a chlorine atom, a hydroxyl group, an iodine atom, a methyl group or a methoxy group, Z.sub.2 is a hydrogen atom; when Z.sub.1 is an amino group, Z.sub.2 is a hydrogen atom or an amino group; when Z.sub.1 is a methyl group, a methoxy group or an amino group, Z.sub.1 is in the 5-position; when Z.sub.1 is an iodine atom, Z.sub.1 is in the 5- or 7-position; and when Z.sub.1 and Z.sub.2 are both amino groups, Z.sub.1 and Z.sub.2 are in the 5- and 7-positions; and the physiologically acceptable acid addition salt thereof which compounds have pharmaceutical utility, e.g.: treating inflammation.

  式(I)的化合物：其中W.sub.1和W.sub.2各自独立地是氢原子或##STR2##基团，其中Y是n-C.sub.1-6烷基烯基或具有C.sub.1-6烷基基团取代物的n-C.sub.1-6烷基烯基；R.sub.1和R.sub.2各自独立地是氢原子或C.sub.1-6烷基基团，以及##STR3##在##STR4##基团中的基团可能形成从吗啡啉，吡咯啉，哌啶，环己哌啶和哌嗪基团中选择的饱和杂环环；除了吗啡啉基团之外的饱和杂环环可能具有至少一个C.sub.1-4烷基基团，羟基基团或卤原子作为取代物；Z.sub.1是氢原子，氯原子，溴原子，碘原子，羟基，氨基，C.sub.1-3烷基基团或甲氧基基团；Z.sub.2是氢原子或氨基；当W.sub.1和W.sub.2都是氢原子时，Z.sub.1是羟基或碘原子，Z.sub.2是氢原子，或Z.sub.1和Z.sub.2都是氨基；当Z.sub.1和Z.sub.2都是氢原子时，W.sub.1或W.sub.2中的##STR5##基团是吗啡啉基团；当Z.sub.1是氯原子，羟基，碘原子，甲基基团或甲氧基基团时，Z.sub.2是氢原子；当Z.sub.1是氨基时，Z.sub.2是氢原子或氨基；当Z.sub.1是甲基基团，甲氧基基团或氨基时，Z.sub.1在5-位；当Z.sub.1是碘原子时，Z.sub.1在5-位或7-位；当Z.sub.1和Z.sub.2都是氨基时，Z.sub.1和Z.sub.2在5-位和7-位；以及其生理上可接受的酸盐，这些化合物具有药用价值，例如：用于治疗炎症。
• Indazole derivatives
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：US04751302A1

  公开（公告）日：1988-06-14

  A compound of the formula (I): ##STR1## wherein W.sub.1 and W.sub.2 each independently is a hydrogen atom or a ##STR2## wherein Y is a n-C.sub.1-6 alkylene group or a n-C.sub.1-6 alkylene group having a C.sub.1-6 alkyl group substituent; and R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-6 alkyl group, and ##STR3## may form a saturated heterocyclic ring selected from the group consisting of morpholino, pyrrolidino, piperidino, homopiperidino and piperazino groups, and the saturated heterocyclic ring except the morpholino group may have at least one C.sub.1-4 alkyl group, hydroxyl group or halogen atom as a substituent; Z.sub.1 is a hydrogen atom, a chlorine atom, a bromine atom, an iodine atom, a hydroxyl group, an amino group, a C.sub.1-3 alkyl group or a methoxy group; Z.sub.2 is a hydrogen atom or an amino group; when W.sub.1 and W.sub.2 are both hydrogen atoms, Z.sub.1 is a hydroxyl group or an iodine atom and Z.sub.2 is hydrogen atom, or Z.sub.1 and Z.sub.2 are both amino groups; when Z.sub.1 and Z.sub.2 are both hydrogen atoms, the ##STR4## in either W.sub.1 or W.sub.2 is a morpholino group; when Z.sub.1 is a chlorine atom, a hydroxyl group, an iodine atom, a methyl group or a methoxy group, Z.sub.2 is a hydrogen atom; when Z.sub.1 is an amino group, Z.sub.2 is a hydrogen atom or an amino group; when Z.sub.1 is a methyl group, a methoxy group or an amino group, Z.sub.1 is in the 5-position; when Z.sub.1 is an iodine atom, Z.sub.1 is in the 5- or 7-position; and when Z.sub.1 and Z.sub.2 are both amino groups, Z.sub.1 and Z.sub.2 are in the 5- and 7-positions; and the physiologically acceptable acid addition salt thereof.

  化合物的公式（I）：##STR1## 其中W.sub.1和W.sub.2各自独立地是氢原子或##STR2##其中Y是n-C.sub.1-6烷基或具有C.sub.1-6烷基取代基的n-C.sub.1-6烷基；R.sub.1和R.sub.2各自独立地是氢原子或C.sub.1-6烷基，且##STR3##可以形成从吗啡啶，吡咯烷，哌啶，同哌啶和哌嗪基中选出的饱和杂环环，除吗啡啶基外的饱和杂环环可以具有至少一个C.sub.1-4烷基，羟基或卤原子作为取代基；Z.sub.1是氢原子，氯原子，溴原子，碘原子，羟基，氨基，C.sub.1-3烷基或甲氧基；Z.sub.2是氢原子或氨基；当W.sub.1和W.sub.2都是氢原子时，Z.sub.1是羟基或碘原子，Z.sub.2是氢原子，或者Z.sub.1和Z.sub.2都是氨基；当Z.sub.1和Z.sub.2都是氢原子时，W.sub.1或W.sub.2中的##STR4##是吗啡啶基；当Z.sub.1是氯原子，羟基，碘原子，甲基或甲氧基时，Z.sub.2是氢原子；当Z.sub.1是氨基时，Z.sub.2是氢原子或氨基；当Z.sub.1是甲基，甲氧基或氨基时，Z.sub.1在5位；当Z.sub.1是碘原子时，Z.sub.1在5位或7位；当Z.sub.1和Z.sub.2都是氨基时，Z.sub.1和Z.sub.2在5位和7位；以及其生理上可接受的酸加成盐。