ethyl 4-(2-furoyl)piperazin-1-ylformimidate hydrochloride | 57200-93-8

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: ethyl 4-(2-furoyl)piperazin-1-ylformimidate hydrochloride
• 英文别名: ethyl 4-(furan-2-carbonyl)piperazine-1-carboximidate;hydrochloride
• CAS: 57200-93-8
• 化学式: C₁₂H₁₇N₃O₃*ClH
• 分子量: 287.746
• InChiKey: SISIVDLMNYYZGO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.43
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  69.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  ethyl 4-(2-furoyl)piperazin-1-ylformimidate hydrochloride 、 2-氨基-4,5-二甲氧基苯腈 以 N,N-二甲基甲酰胺 、 mineral oil 为溶剂， 生成 哌唑嗪
  参考文献：
  名称：

  Process for hypotensive 4-amino-2-(piperazin-1-yl) quinazoline

  摘要：

  6,7-二甲氧基-4-氨基-2-(4-取代哌嗪-1-基)-喹唑啉和6,7,8-三甲氧基-4-氨基-2-(4-取代哌嗪-1-基)喹唑啉可以通过以下两种方法制备：(1)将适当的4,5-二甲氧基或3,4,5-三甲氧基取代的2-氨基苯甲腈与某些1,4-二取代哌嗪反应；或(2)将适当的4,5-二甲氧基或3,4,5-三甲氧基取代的2-氨基苯甲酰胺与相同的1,4-二取代哌嗪反应。这些产物是已知的降压剂。

  公开号：

  US03935213A1

文献信息

• Alkoxy-substituted-6-chloro-quinazoline-2,4-diones
  申请人：Pfizer Inc.

  公开号：US04287341A1

  公开（公告）日：1981-09-01

  2,4-Diaminoquinazolines of the formula ##STR1## wherein Y.sup.1 is hydrogen or chloro, Y.sup.2 is OR, Y.sup.3 is hydrogen or OR such that when Y.sup.1 is hydrogen, Y.sup.3 is OR and when Y.sup.1 is chloro, Y.sup.3 is hydrogen or OR, and the pharmaceutically acceptable salts thereof; R represents an alkyl group having from one to three carbon atoms; taken separately, R.sup.1 and R.sup.2 are each hydrogen, alkyl having from one to five carbon atoms, cycloalkyl having from three to eight carbon atoms, alkenyl or alkynyl each having from three to five carbon atoms or hydroxy substituted alkyl having from two to five carbon atoms, when taken together with the nitrogen atom to which they are attached R.sup.1 and R.sup.2 form a substituted or unsubstituted heterocyclic group optionally containing an atom of oxygen, sulfur or a second atom of nitrogen as a ring member; their use as antihypertensive agents, pharmaceutical compositions containing them and intermediates for their production.

  2,4-二氨基喹唑啉的化学式为##STR1##，其中Y.sup.1为氢或氯，Y.sup.2为OR，Y.sup.3为氢或OR，当Y.sup.1为氢时，Y.sup.3为OR，当Y.sup.1为氯时，Y.sup.3为氢或OR，以及其药用盐；R代表一个具有一至三个碳原子的烷基基团；单独取R.sup.1和R.sup.2分别为氢、具有一至五个碳原子的烷基、具有三至八个碳原子的环烷基、具有三至五个碳原子的烯基或炔基，或具有两至五个碳原子的羟基取代的烷基，当与它们连接的氮原子一起时，R.sup.1和R.sup.2形成一个取代或未取代的杂环基团，该基团可选地含有一个氧原子、硫原子或第二个氮原子作为环成员；它们作为降压药剂的用途，含有它们的药物组合物以及它们生产的中间体。
• Chloro- and alkoxy-substituted-2-chloro-4-aminodquinazolines
  申请人：Pfizer Inc.

  公开号：US04351940A1

  公开（公告）日：1982-09-28

  2,4-Diaminoquinazolines of the formula ##STR1## wherein Y.sup.1 is hydrogen or chloro, Y.sup.2 is OR, Y.sup.3 is hydrogen or OR such that when Y.sup.1 is hydrogen, Y.sup.3 is OR and when Y.sup.1 is chloro, Y.sup.3 is hydrogen or OR, and the pharmaceutically acceptable salts thereof; R represents an alkyl group having from one to three carbon atoms; taken separately, R.sup.1 and R.sup.2 are each hydrogen, alkyl having from one to five carbon atoms, cycloalkyl having from three to eight carbon atoms, alkenyl or alkynyl each having from three to five carbon atoms or hydroxy substituted alkyl having from two to five carbon atoms, when taken together with the nitrogen atom to which they are attached R.sup.1 and R.sup.2 form a substituted or unsubstituted heterocyclic group optionally containing an atom of oxygen, sulfur or a second atom of nitrogen as a ring member; their use as antihypertensive agents, pharmaceutical compositions containing them and intermediates for their production.

  公式为 ##STR1## 的2,4-二氨基喹嗪，其中Y1为氢或氯，Y2为OR，Y3为氢或OR，当Y1为氢时，Y3为OR，当Y1为氯时，Y3为氢或OR，以及其药学上可接受的盐；R代表具有1至3个碳原子的烷基；分别取R1和R2为氢、具有1至5个碳原子的烷基、具有3至8个碳原子的环烷基、具有3至5个碳原子的烯基或炔基或具有2至5个碳原子的羟基取代的烷基，当它们与它们所连接的氮原子一起取用时，R1和R2形成一个取代或未取代的杂环基，可选地含有一个氧原子、硫原子或第二个氮原子作为环成员；它们作为降压剂的用途，包含它们的制药组合物和它们制备的中间体。
• Chloro- and alkoxy-substituted-2,4-diaminoquinazolines
  申请人：Pfizer Inc.

  公开号：US04377581A1

  公开（公告）日：1983-03-22

  2,4-Diaminoquinazolines of the formula ##STR1## wherein Y.sup.1 is hydrogen or chloro, Y.sup.2 is OR, Y.sup.3 is hydrogen or OR such than when Y.sup.1 is hydrogen, Y.sup.3 is OR and when Y.sup.1 is chloro, Y.sup.3 is hydrogen or OR, and the pharmaceutically acceptable salts thereof; R represents an alkyl group having from one to three carbon atoms; taken separately, R.sup.1 and R.sup.2 are each hydrogen, alkyl having from one to five carbon atoms, cycloalkyl having from three to eight carbon atoms, alkenyl or alkynyl each having from three to five carbon atoms or hydroxy substituted alkyl having from two to five carbon atoms, when taken together with the nitrogen atom to which they are attached R.sup.1 and R.sup.2 form a substituted or unsubstituted heterocyclic group optionally containing an atom of oxygen, sulfur or a second atom of nitrogen as a ring member; their use as antihypertensive agents, pharmaceutical compositions containing them and intermediates for their production.

  该专利描述了式子##STR1##中Y.sup.1是氢或氯，Y.sup.2是OR，Y.sup.3是氢或OR，当Y.sup.1是氢时，Y.sup.3是OR，当Y.sup.1是氯时，Y.sup.3是氢或OR。其中R代表一个由一个到三个碳原子组成的烷基；R.sup.1和R.sup.2分别为氢、由一个到五个碳原子组成的烷基、由三到八个碳原子组成的环烷基、由三到五个碳原子组成的烯基或炔基或在有机取代的情况下，为由两个到五个碳原子组成的羟基取代的烷基。当它们与它们所连接的氮原子一起取代时，R.sup.1和R.sup.2形成一个取代或未取代的杂环基，该杂环基可以选择性地包含一个氧原子、硫原子或第二个氮原子作为环成员。该专利还涉及这些化合物作为降压剂的用途，包含它们的制药组合物以及它们的中间体的生产。
• Chloro- and alkoxy-substituted-2,4-diaminoquinazolines and pharmaceutical compositions containing them
  申请人：PFIZER INC.

  公开号：EP0028473A1

  公开（公告）日：1981-05-13

  2,4-Diaminoquinazolinesoftheformula: and the pharmaceutically acceptable salts thereof are disclosed and claimed as novel compounds having useful antihypertensive activity wherein: Y' is hydrogen or chloro, Y2 is OR and Y' is hydrogen or OR, such that when Y' is hydrogen, Y3 is OR and when Y' is chloro, Y3 is hydrogen or OR; R represents an alkyl group having from one to three carbon atoms; when taken separately, R1 and R2 are each hydrogen, alkyl having from one to five carbon atoms, cycloalkyl having from three to eight carbon atoms, alkenyl or alkynyl each having from three to five carbon atoms or hydroxy substituted alkyl having from two to five carbon atoms; when taken together with the nitrogen atom to which they are attached, R and R2 form any one of a number of specified substituted or unsubstituted heterocyclic groups optionally containing also an atom of oxygen, sulfur or a second atom of nitrogen as a ring member. Also disclosed and claimed are pharmaceutical compositions containing such compounds, and novel intermediates for their production, having the formulae: and

  2,4-Diaminoquinazolinesoftheformula： 及其药学上可接受的盐类公开并声称是具有有用的抗高血压活性的新型化合物，其中：Y'是氢或氯，Y2是OR，Y'是氢或OR，这样，当Y'是氢时，Y3是OR，当Y'是氯时，Y3是氢或OR；R代表具有1至3个碳原子的烷基；当单独使用时，R1和R2各自是氢、具有1至5个碳原子的烷基、具有3至8个碳原子的环烷基、各自具有3至5个碳原子的烯基或炔基或具有2至5个碳原子的羟基取代的烷基；当 R 和 R2 与它们所连接的氮原子结合在一起时，R 和 R2 形成若干指定的取代或未取代的杂环基团中的任一个，这些杂环基团还可选择含有一个氧原子、硫原子或第二个氮原子作为环成员。本发明还公开了含有此类化合物的药物组合物，以及用于生产此类化合物的新型中间体，其结构式为 和
• US3935213A
  申请人：——

  公开号：US3935213A

  公开（公告）日：1976-01-27