1-Ethoxycarbonyl-5-phenyl-2-pyrazoline | 124330-05-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 1-Ethoxycarbonyl-5-phenyl-2-pyrazoline
• 英文别名: 5-phenyl-4,5-dihydro-pyrazole-1-carboxylic acid ethyl ester；5-Phenyl-4,5-dihydro-pyrazol-1-carbonsaeure-aethylester；ethyl 3-phenyl-3,4-dihydropyrazole-2-carboxylate
• CAS: 124330-05-8
• 化学式: C₁₂H₁₄N₂O₂
• 分子量: 218.255
• InChiKey: PJLJTYCTXHSVAA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  41.9
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  氯甲酸乙酯 、 alkaline earth salt of/the/ methylsulfuric acid 在 吡啶 作用下， 生成 1-Ethoxycarbonyl-5-phenyl-2-pyrazoline
  参考文献：
  名称：

  v. Auwers; Heimke, Justus Liebigs Annalen der Chemie, 1927, vol. 458, p. 209

  摘要：

  DOI：

文献信息

• Pyrazoline derivatives for treating cerebrovascular diseases
  申请人：Mitsui Toatsu Chemicals, Inc.

  公开号：US04839376A1

  公开（公告）日：1989-06-13

  2-Pyrazoline derivatives of the formula (A): ##STR1## where R.sup.1 is a pyridyl, a pyrazyl or an alkoxy group; and R.sup.2 is a hydrogen atom, an alkyl, a pyridyl, a furyl, phenyl or a substituted phenyl group, and to a process for producing the same. Therapeutic agents for treating cerebrovascular diseases containing, as the active ingredient, a 2-pyrazoline derivative represented by the formula (G): ##STR2## where R.sup.3 is a hydrogen atom, an alkyl, acetyl, an alkoxycarbonyl, an amino, benzoyl, a substituted benzoyl, a pyridylcarbonyl, a furylcarbonyl, a thienylcarbonyl, a pyrazylcarbonyl, an N-substituted carbamoyl, an N-substituted thiocarbamoyl, or carboxy group; and R.sup.4 is a hydrogen atom, an alkyl, a pyridyl, a thienyl, a furyl, cyclohexyl, phenyl or a substituted phenyl group or a pharmaceutically acceptable salt thereof. These therapeutic agents cope with cerebral edemas in the acute stage of cerebral apoplexy and regulates the whole-body and intracranial body circulation, thereby protecting ischemic lesions and minimizing the spread to affected parts.

  2-吡唑啉衍生物的化学式（A）：##STR1##其中R.sup.1是吡啶基，吡唑基或烷氧基；R.sup.2是氢原子，烷基，吡啶，呋喃基，苯基或取代苯基，以及制备这些化合物的方法。治疗脑血管疾病的药物，其活性成分是由化学式（G）表示的2-吡唑啉衍生物：##STR2##其中R.sup.3是氢原子，烷基，乙酰基，烷氧羰基，氨基，苯甲酰基，取代苯甲酰基，吡啶羰基，呋喃羰基，噻吩羰基，吡唑基羰基，N-取代氨基甲酰基，N-取代硫氨基甲酰基或羧基；R.sup.4是氢原子，烷基，吡啶，噻吩，呋喃，环己基，苯基或取代苯基或其药用可接受盐。这些治疗药物用于急性脑卒中的脑水肿，并调节全身和颅内循环，从而保护缺血病变并最小化蔓延到受影响部位。
• Pyrazolone derivatives for treating cerebrovascular diseases
  申请人：Mitsui Toatsu Chemicals

  公开号：US04990529A1

  公开（公告）日：1991-02-05

  2-Pyrazoline derivatives of the formula (A): ##STR1## where R.sup.1 is a pyridyl, a pyrazyl or an alkoxyl group; and R.sup.2 is a hydrogen atom, an alkyl, a pyridyl, a furyl, phenyl or a substituted phenyl group, and to a process for producing the same. Therapeutic agents for treating cerebrovascular diseases containing, as the active ingredient, a 2-pyrazoline derivative represented by the formula (G): ##STR2## where R.sup.3 is a hydrogen atom, an alkyl, acetyl, an alkoxycarbonyl, an amino, benzoyl, a substituted benzoyl, a pyridylcarbonyl, a furylcabonyl, a thienylcarbonyl, a pyrazylocarbonyl, an N-substituted carbamoyl, an N-substituted thiocarbamoyl, or carboxyl group; and R.sup.4 is a hydrogen atom, an alkyl, a pyridyl, a thienyl, a furyl, cyclohexyl, phenyl or a substituted phenyl group or a pharmaceutically acceptable salt thereof. These therapeutic agents cope with cerebral edemas in the acute stage of cerebral apoplexy and regulates the whole-body and intracranial body circulation, thereby protecting ischemic lesions and minimizing the spread to affected parts.

  化学式为(A)的2-吡唑烷衍生物：##STR1## 其中R.sup.1是吡啶基，吡唑基或烷氧基；R.sup.2是氢原子，烷基，吡啶基，呋喃基，苯基或取代苯基，并提供一种制备它们的方法。治疗脑血管疾病的药物，其活性成分为2-吡唑烷衍生物，化学式为(G)：##STR2## 其中R.sup.3是氢原子，烷基，乙酰基，烷氧羰基，氨基，苯甲酰基，取代苯甲酰基，吡啶基羰基，呋喃基羰基，噻吩基羰基，吡唑基羰基，N-取代氨基甲酰基，N-取代硫代氨基甲酰基或羧基；R.sup.4是氢原子，烷基，吡啶基，噻吩基，呋喃基，环己基，苯基或取代苯基或其药学上可接受的盐。这些治疗剂对于急性脑卒中的脑水肿有作用，并调节全身和颅内循环，从而保护缺血损伤并最小化对受影响部位的扩散。
• Pyrazoline derivatives and agents for treating cerebrovascular diseases containing the same as active ingredient
  申请人：MITSUI TOATSU CHEMICALS, Inc.

  公开号：EP0295695A2

  公开（公告）日：1988-12-21

  This invention relates to new 2-pyrazoline derivatives represented by the following general formula (A): ( wherein R¹ denotes a pyridyl, a pyrazyl or an alkoxyl group; and R² stands for hydrogen atom, an alkyl, a pyridyl, a furyl, phenyl or a substituted phenyl group ), and to a process for producing the same. This invention also relates to agents for treating cerebrovascular diseases containing, as active ingredients, a 2-pyrazoline derivative represented by the following general formula (G): ( wherein R³ denotes hydrogen atom, an alkyl, acetyl, an alkoxycarbonyl, an amino, benzoyl, a substituted benzoyl, a pyridylcarbonyl, a furylcabonyl, a thienylcarbonyl, a pyrazylcarbonyl, an N-substituted carbamoyl, an N-sub­stituted thiocarbamoyl, or carboxyl group; and R⁴ stands for hydrogen atom, an alkyl, a pyridyl, a thienyl, a furyl, cyclohexyl, phenyl or a substituted phenyl group ) or a pharmaceutically acceptable salt thereof. Administration of an agent of this invention for treat­ing cerebrovascular diseases copes with cerebral edemata in the acute stage of cerebral apoplexy and regulates the whole-body and intracranial blood circulation, thereby protecting ischemic lesions and minimizing the spread of affected parts.

  本发明涉及由以下通式(A)代表的新的 2-吡唑啉衍生物： (其中，R¹表示吡啶基、吡嗪基或烷氧基；R²表示氢原子、烷基、吡啶基、呋喃基、苯基或取代苯基），并涉及其生产工艺。本发明还涉及治疗脑血管疾病的制剂，其活性成分含有下通式（G）代表的 2-吡唑啉衍生物： (其中 R³ 表示氢原子、烷基、乙酰基、烷氧羰基、氨基、苯甲酰基、取代苯甲酰基、吡啶羰基、呋喃羰基、噻吩羰基、吡嗪羰基、N-取代氨基甲酰基、N-取代硫代氨基甲酰基或羧基；R⁴代表氢原子、烷基、吡啶基、噻吩基、呋喃基、环己基、苯基或取代苯基）或其药学上可接受的盐。 服用本发明治疗脑血管疾病的制剂，可在脑中风的急性期处理脑水肿，调节全身和颅内血液循环，从而保护缺血性病变，最大限度地减少受影响部位的扩散。
• Process for producing 1-acyl-2-pyrazoline derivatives
  申请人：MITSUI TOATSU CHEMICALS, Inc.

  公开号：EP0322691A1

  公开（公告）日：1989-07-05

  1-Acyl-2-pyrazoline derivatives represented by the formula where R¹ denotes a hydrogen atom, pyridyl group, pyrazinyl group, alkyl group, aryl group, or alkoxy group; and R², R³, and R⁴ independently denote a hydrogen atom, furyl group, pyridyl group, alkyl group, or aryl group, are produced by cyclizing by heating an acylhydrazone derivative represented by the formula where R¹, R², R³, and R⁴ are defined as above, to produce compounds having useful anti-cerebral edema activity.

  1-酰基-2-吡唑啉衍生物，由式表示 式中 R¹表示氢原子、吡啶基、吡嗪基、烷基、芳基或烷氧基；R²、R³和R⁴独立地表示氢原子、糠基、吡啶基、烷基或芳基，通过加热环化由式表示的酰基腙衍生物而制得。 其中 R¹、R²、R³ 和 R⁴ 的定义同上，从而制得具有有效抗脑水肿活性的化合物。
• YAMASHITA, HIROYUKI;ODATE, MAKOTO;IIZUKA, HAJIME;KAWAZURA, HIROSHI;SHIGA,+
  作者：YAMASHITA, HIROYUKI、ODATE, MAKOTO、IIZUKA, HAJIME、KAWAZURA, HIROSHI、SHIGA,+

  DOI：——

  日期：——