1-氨基-4-苯基哌嗪 | 14340-32-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 中文名称: 1-氨基-4-苯基哌嗪
• 中文别名: 4-苯基哌嗪-1-胺；(4-苯基哌嗪-1-基)胺；4-苯基-1-哌嗪胺
• 英文名称: 4-phenylpiperazin-1-amine
• CAS: 14340-32-0
• 化学式: C₁₀H₁₅N₃
• mdl: MFCD07364280
• 分子量: 177.249
• InChiKey: DAURIJZNKHAJSE-UHFFFAOYSA-N

物化性质

• 熔点：
  53-55 °C
• 沸点：
  125-130 °C(Press: 1 Torr)
• 密度：
  1.105

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  32.5
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2933599090

反应信息

• 作为反应物：
  描述：

  1-氨基-4-苯基哌嗪 在 potassium carbonate 作用下， 以 乙醇 、 苯 为溶剂， 反应 6.0h， 生成 1-(2-Dimethylamino-ethyl)-3-(4-methoxy-phenyl)-1-(4-phenyl-piperazin-1-yl)-thiourea
  参考文献：
  名称：

  Ahmad; Yasmeen; Saxena, Journal of the Indian Chemical Society, 1985, vol. 62, # 3, p. 241 - 243

  摘要：

  DOI：
• 作为产物：
  描述：

  N-苯基哌嗪 在 lithium aluminium tetrahydride 、 亚硝酸特丁酯 作用下， 以 四氢呋喃 为溶剂， 反应 3.0h， 生成 1-氨基-4-苯基哌嗪
  参考文献：
  名称：

  Structure–activity studies in the development of a hydrazone based inhibitor of adipose-triglyceride lipase (ATGL)

  摘要：

  Adipose triglyceride lipase (ATGL) catalyzes the degradation of cellular triacylglycerol stores and strongly determines the concentration of circulating fatty acids (FAs). High serum FA levels are causally linked to the development of insulin resistance and impaired glucose tolerance, which eventually progresses to overt type 2 diabetes. ATGL-specific inhibitors could be used to lower circulating FAs, which can counteract the development of insulin resistance. In this article, we report about structure-activity relationship (SAR) studies of small molecule inhibitors of ATGL based on a hydrazone chemotype. The SAR indicated that the binding pocket of ATGL requests rather linear compounds without bulky substituents. The best inhibitor showed an IC50 = 10 mu M in an assay with COS7-cell lysate overexpressing murine ATGL. (C) 2015 The Authors. Published by Elsevier Ltd. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).

  DOI：

  10.1016/j.bmc.2015.02.051

文献信息

• [EN] 4- BROMO - 5 - (2- CHLORO - BENZOYLAMINO) - 1H - PYRAZOLE - 3 - CARBOXYLIC ACID AMIDE DERIVATIVES AND RELATED COMPOUNDS AS BRADYKININ B1 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES<br/>[FR] DERIVES AMIDES DE L'ACIDE CARBOXYLIQUE DE 4- BROMO - 5 - (2- CHLORO - BENZOYLAMINO) - 1H - PYRAZOLE 3 ET COMPOSES ASSOCIES EN TANT QU'ANTAGONISTES DE RECEPTEUR DE B1 DE LA BRADYKININE POUR LE TRAITEMENT DE MALADIES INFLAMMATOIRES
  申请人：ELAN PHARM INC

  公开号：WO2004098589A1

  公开（公告）日：2004-11-18

  Disclosed are compounds of formula I and II that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action.

  公开的是化合物I和II的结构式，它们是激肽酶B1受体拮抗剂，适用于治疗哺乳动物中由激肽酶B1受体介导的疾病，或缓解与疾病状况相关的不良症状。其中某些化合物表现出增强的效力，并且预计还将表现出延长作用的特性。
• [EN] NEW DRUGS WITH ANTICHOLESTATIC ACTIVITY<br/>[FR] NOUVEAUX MÉDICAMENTS À ACTION ANTI-CHOLESTATIQUE
  申请人：SEGIX ITALIA S R L

  公开号：WO2009010555A1

  公开（公告）日：2009-01-22

  New compounds belonging to the structural formula (I) are described. formula (I) in which R1, R2, A, Y and X are specified in the description, useful in the treatment of cholestasis and substantially devoid of antibacterial activity. The synthesis process of said compounds, the pharmaceutical compositions containing them and their use in therapy are also described.

  描述了属于结构式（I）的新化合物。 公式（I）中R1、R2、A、Y和X在描述中指定，适用于治疗胆汁淤积且基本上不具有抗菌活性。 还描述了这些化合物的合成过程、含有它们的药物组成物以及它们在治疗中的用途。
• DRUGS WITH ANTICHOLESTATIC ACTIVITY
  申请人：Brufani Mario

  公开号：US20100168129A1

  公开（公告）日：2010-07-01

  New compounds belonging to the structural formula (I) are described. in which R1, R2, A, Y and X are specified in the description, useful in the treatment of cholestasis and substantially devoid of antibacterial activity. The synthesis process of said compounds, the pharmaceutical compositions containing them and their use in therapy are also described.

  描述了属于结构式（I）的新化合物，其中R1、R2、A、Y和X在描述中有具体规定，适用于治疗胆汁淤积症且基本上不具有抗菌活性。还描述了所述化合物的合成过程、含有它们的药物组合物以及它们在治疗中的用途。
• [EN] PREGNANE-OXIMINO-AMINOALKYLETHERS AND PROCESS FOR PREPARATION THEREOF, USEFUL AS ANTIDIABETIC AND ANTIDYSLIPIDEMIC AGENTS<br/>[FR] PRÉGNANE-OXIMINO-AMINOALKYLÉTHERS ET PROCÉDÉ DE PRÉPARATION DE CEUX-CI, UTILES EN TANT QU'AGENTS ANTIDIABÉTIQUES ET ANTIDYSLIPIDÉMIANTS
  申请人：COUNCIL SCIENT IND RES

  公开号：WO2014115170A1

  公开（公告）日：2014-07-31

  The present invention relates to the synthesis of pregnane-oximino-aminoalkyl-ethers and their antidiabetic and antidyslipidemic activities. More particularly, the invention relates to the synthesis of compounds of formula 3 and biological profile thereof. Further the invention relates to compounds of formula 3 and pharmaceutically acceptable salts thereof.

  本发明涉及孕烷-肟基-氨基烷基醚类化合物的合成及其抗糖尿病和抗血脂异常活性。更具体地，本发明涉及化合物3的合成及其生物学特性。此外，本发明还涉及化合物3及其药用可接受盐。
• Selective reduction of N-nitroso aza-aliphatic cyclic compounds to the corresponding N-amino products using zinc dust in CO2–H2O medium
  作者：Weiqing Yang、Xiang Lu、Tingting Zhou、Yongjing Cao、Yuanyuan Zhang、Menglin Ma

  DOI：10.1007/s10593-018-2349-0

  日期：2018.8

  A new method for reduction of N-nitroso aza-aliphatic cyclic compounds employing zinc in pressurized CO2–H2O medium has been developed. H2O and NH4Cl were used as hydrogen donors, and reduction was performed under environmentally benign conditions. The presented approach allowed to obtain the respective N-amino products selectively and in excellent yields (up to 97%).

  开发了一种在加压的CO 2 -H 2 O介质中使用锌还原N-亚硝基氮杂-脂族环状化合物的新方法。使用H 2 O和NH 4 Cl作为氢供体，并在环境良好的条件下进行还原。提出的方法允许选择性地并且以优异的产率（高达97％）获得各个N-氨基产物。