N-(2-hydroxy-phenyl)-formamidine | 53150-18-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 酚类
• 英文名称: N-(2-hydroxy-phenyl)-formamidine
• 英文别名: N-(o-hydroxyphenyl)-formamidine；N'-(2-hydroxyphenyl)methanimidamide
• CAS: 53150-18-8
• 化学式: C₇H₈N₂O
• mdl: MFCD19206950
• 分子量: 136.153
• InChiKey: RIUDNNWBQBNYQY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  58.6
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-(2-hydroxy-phenyl)-formamidine 150.0 ℃ 、1.33 Pa 条件下， 生成 苯并恶唑
  参考文献：
  名称：

  Investigation of the synthesis of benzoxazole via aryne reaction

  摘要：

  DOI：

  10.1021/jo00329a022
• 作为产物：
  描述：

  N-(2-氯苯基)-甲酰胺 在 potassium amide 作用下， 以 氨 为溶剂， 反应 1.0h， 生成 N-(2-hydroxy-phenyl)-formamidine
  参考文献：
  名称：

  Investigation of the synthesis of benzoxazole via aryne reaction

  摘要：

  DOI：

  10.1021/jo00329a022

文献信息

• N-hydroxyformamidine derivatives
  申请人：Sato Masakazu

  公开号：US20060004078A1

  公开（公告）日：2006-01-05

  An N-hydroxyformamidine derivative of the following formula or a pharmaceutically acceptable salt thereof: (wherein R 1 represents a hydrogen atom, a C 1-4 alkyl group, a C 1-4 alkoxy group or a halogen atom, A represents a C 1-10 alkylene group or a group of the following formula: (wherein m, n and p each represent an integer of 0 to 4), and R represents an N,N-di-C 1-6 alkylamino group, a dioxanyl group, a C 1-4 alkyl-substituted dioxanyl group, a C 1-4 alkoxy-C 1-4 alkoxy group or a group of the following formula: (wherein s and t each represent an integer of 1 to 4, B represents a methylene group, an oxygen atom, a sulfur atom, a nitrogen atom, a C 1-4 alkyl-substituted nitrogen atom, a phenyl-substituted nitrogen atom or a benzyl-substituted nitrogen atom, R 2 represents a hydrogen atom or a C 1-4 alkyl group, and r represents an integer of 0 to 2)). The present invention aims to provide an agent for inhibiting 20-HETE-producing enzymes, 20-HETE being involved in the effects of causing microvascular constriction or dilation in major organs (e.g., kidneys, cerebral blood vessels) or of inducing cell proliferation, etc.

  该N-羟基甲酰胺衍生物具有以下结构式或其药用盐：（其中R1代表氢原子、C1-4烷基、C1-4甲氧基或卤素原子，A代表C1-10烷基或以下结构式的基团：（其中m、n和p分别表示0至4的整数），R代表N,N-二C1-6烷基氨基、二氧杂环丙基、C1-4烷基取代的二氧杂环丙基、C1-4甲氧基-C1-4甲氧基或以下结构式的基团：（其中s和t分别表示1至4的整数，B代表亚甲基、氧原子、硫原子、氮原子、C1-4烷基取代的氮原子、苯基取代的氮原子或苄基取代的氮原子，R2代表氢原子或C1-4烷基，r表示0至2的整数）。本发明旨在提供一种抑制20-HETE产生酶的药剂，20-HETE参与引起主要器官（如肾脏、脑血管）微血管收缩或扩张的效应，或诱导细胞增殖等。
• El-Meligy,M.S.A.; Mohamed,S.A., Journal fur praktische Chemie (Leipzig 1954), 1974, vol. 316, p. 154 - 158
  作者：El-Meligy,M.S.A.、Mohamed,S.A.

  DOI：——

  日期：——
• EL-SHEIKH, MUSTAFA, I.;MARKS, A.;BIEHL, E. R., J. ORG. CHEM., 1981, 46, N 16, 3256-3259
  作者：EL-SHEIKH, MUSTAFA, I.、MARKS, A.、BIEHL, E. R.

  DOI：——

  日期：——
• US7288566B2
  申请人：——

  公开号：US7288566B2

  公开（公告）日：2007-10-30
• [EN] SPHINGOSINE-1-PHOSPATE RECEPTOR MODULATORS FOR TREATMENT OF CARDIOPULMONARY DISORDERS<br/>[FR] MODULATEURS DU RÉCEPTEUR DE LA SPHINGOSINE -1-PHOSPHATE POUR LE TRAITEMENT DE TROUBLES CARDIO-PULMONAIRES
  申请人：SCRIPPS RESEARCH INST

  公开号：WO2016053855A1

  公开（公告）日：2016-04-07

  The invention provides compounds effective as sphingosine-1 -phosphate receptor modulators for treatment of cardiopulmonary diseases, such as hypertension (including malignant hypertension), angina, myocardial infarction, cardiac arrhythmias, congestive heart failure, coronary heart disease, atherosclerosis, angina pectoris, dysrhythmias, cardiomyothopy (including hypertropic cardiomyothopy), heart failure, cardiac arrest, bronchitis, asthma, chronic obstructive pulmonary disease, cystic fibrosis, croup, emphysema, pleurisy, pulmonary fibrosis, pneumonia, pulmonary embolus, pulmonary hypertension, mesothelioma, ventricular conduction abnormalities, complete heart block, adult respiratory distress syndrome, sepsis syndrome, idiopathic pulmonary fibrosis, scleroderma, systemic sclerosis, retroperitoneal fibrosis, prevention of keloid formation, or cirrhosis.