1-(4-甲氧基苯基)-2-甲基-哌嗪 | 35947-12-7

• 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-(4-甲氧基苯基)-2-甲基-哌嗪
• 中文别名: 1-(4-甲氧基苯基)-3-甲基哌嗪
• 英文名称: 1-(4-methoxyphenyl)-2-methylpiperazine
• CAS: 35947-12-7
• 化学式: C₁₂H₁₈N₂O
• 分子量: 206.288
• InChiKey: LSIROHVGZARUJC-UHFFFAOYSA-N

物化性质

• 沸点：
  345.15°C (rough estimate)
• 密度：
  1.0310 (rough estimate)

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  24.5
• 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-(4-甲氧基苯基)-2-甲基-哌嗪 以 甲醇 、 乙醇 为溶剂， 反应 48.0h， 生成 5-<1-(4-methoxyphenyl)-4-(2-methyl)piperazino>methyl-2-amino-2-oxazoline
  参考文献：
  名称：

  Synthesis and antidepressant activity of 5-(1-aryl-4-piperazino)methyl-2-amino-2-oxazolines

  摘要：

  The synthesis of 20 5-(1-aryl-4-piperazino)methyl-2-amino-2-oxazolines is described. Antidepressant activity was observed in mice using classical screening tests. Structure-activity relationships were studied and correlated with the nature of the aromatic substituent. Preliminary lipophilic and electronic properties of one lead compound (COR 3224) have been described.

  DOI：

  10.1016/0223-5234(92)90177-3
• 作为产物：
  描述：

  硫酸 、 1-(4-Methoxyphenyl)-2-methyl-4-(4-methylphenylsulfonyl)piperazine 、 sodium hydroxide 在 ice 、 4-甲基-2-戊酮 、 potassium carbonate 作用下， 以 水 为溶剂， 反应 20.0h， 以yielding 1.7 parts of oily 1-(4-methoxyphenyl)-2-methylpiperazine的产率得到1-(4-甲氧基苯基)-2-甲基-哌嗪
  参考文献：
  名称：

  [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-diox

  摘要：

  替代[[4-[4-(4-苯基-1-哌嗪基)苯氧甲基]-1,3-二氧杂环戊烷-2-基]甲基]-1H-咪唑和1H-1,2,4-三唑具有抗微生物性质，特别适用于治疗阴道念珠菌病。

  公开号：

  US04619931A1

文献信息

• Carboxylic acid derivatives, medicaments comprising these compounds,
  申请人：Karl Thomae

  公开号：US05994356A1

  公开（公告）日：1999-11-30

  The present invention relates to carboxylic acid derivatives of the general formula ##STR1## in which R.sub.a to R.sub.c, A, B, D, E and X.sub.1 to X.sub.3 are as defined in claim 1, their tautomers, their stereoisomers including their mixtures, and their salts, in particular their physiologically tolerated salts with inorganic or organic acids or bases, which have useful pharmacological properties, preferably aggregation-inhibiting inhibiting actions, medicaments containing these compounds, their use and processes for their preparation.

  本发明涉及一般式##STR1##的羧酸衍生物，其中R.sub.a至R.sub.c，A，B，D，E和X.sub.1至X.sub.3如权利要求1所定义，它们的互变异构体，它们的立体异构体包括它们的混合物，以及它们的盐，特别是它们与无机或有机酸或碱的生理耐受盐，具有有用的药理特性，优选具有聚集抑制作用的药物，含有这些化合物的药物，它们的用途和制备方法。
• [EN] N-PHENYL-PIPERAZINE DERIVATIVES AND METHODS OF PROPHYLAXIS OR TREATMENT OF 5HT2C RECEPTOR ASSOCIATED DISEASES<br/>[FR] DERIVES DE N-PHENYL-PIPERAZINE ET METHODES DE PROPHYLAXIE OU DE TRAITEMENT DE MALADIES ASSOCIEES AU RECEPTEUR 5HT2C
  申请人：ARENA PHARM INC

  公开号：WO2005016902A1

  公开（公告）日：2005-02-24

  The present invention relates to certain substituted N-phenyl-piperazine derivatives of Formula: (I) that are modulators of the 5HT2c receptor. Accordingly, compounds of the present invention are useful for the prophylaxis or treatment of 5HT2c receptor associated diseases or disorders, such as, obesity, Alzheimer Disease, erectile dysfunction and related disorders.

  本发明涉及某些Formula: (I)的取代N-苯基哌嗪衍生物，它们是5HT2c受体的调节剂。因此，本发明的化合物对于预防或治疗与5HT2c受体相关的疾病或紊乱，如肥胖症、阿尔茨海默病、勃起功能障碍及相关疾病，是有用的。
• Substituted 4,5,6,7-tetrahydrobenzthiazol-2-ylamine compounds
  申请人：Oberboersch Stefan

  公开号：US20070027315A1

  公开（公告）日：2007-02-01

  Substituted 4,5,6,7-tetrahydrobenzothiazol-2-ylamine compounds, a method for their production; pharmaceutical compositions comprising them, and methods of use for modulating biological functions and/or treating or inhibiting various medical conditions such as, e.g., depression and pain.

  4,5,6,7-四氢苯并噻唑-2-胺化合物的替代物，其生产方法；包括它们的药物组合物，以及用于调节生物功能和/或治疗或抑制各种医疗状况（如抑郁症和疼痛等）的使用方法。
• [[4
  申请人：Janssen Pharmaceutica, N.V.

  公开号：US04735942A1

  公开（公告）日：1988-04-05

  Substituted [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3 dioxolan-2-yl]methyl]-1H-imidazoles and 1H-1,2,4-triazoles having antimicrobial properties and being particularly useful in the treatment of vaginal candidosis.

  替代品[[4-[4-(4-苯基-1-哌嗪基)苯氧甲基]-1,3-二氧杂环戊烷-2-基]甲基]-1H-咪唑和1H-1,2,4-三唑具有抗微生物性能，特别适用于治疗阴道念珠菌病。
• Aromatic sulfone hydroxamic acid metalloprotease inhibitor
  申请人：Barta E. Thomas

  公开号：US20060084688A1

  公开（公告）日：2006-04-20

  A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9, and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein R 1 and R 2 are both hydrido or R 1 and R 2 together with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. R 3 in formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.

  本发明揭示了一种治疗方法，包括向患有与病理性基质金属蛋白酶活性相关的病症的宿主施用一种具有出色的抑制一种或多种基质金属蛋白酶（MMP）酶活性的芳香磺酰羟肟酸有效量，例如MMP-2、MMP-9和MMP-13，同时在至少MMP-1方面表现出显著较少的抑制作用。所施用的酶抑制剂在结构上对应于下式（I）或其药学上可接受的盐，其中R1和R2均为氢基或R1和R2与它们键合的原子形成一个5到8个成员环，该环中含有一个、两个或三个杂原子，该杂原子为氧、硫或氮。式（I）中的R3为可选的取代芳基或可选的取代杂芳基基团。本发明还揭示了具有这些选择性活性的金属蛋白酶抑制剂化合物，制造这种化合物的过程以及使用抑制剂的制药组合物。