1-(2-fluorophenyl)-4-methylpiperazine | 218940-65-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 1-(2-fluorophenyl)-4-methylpiperazine
• 英文别名: 1-(2-Fluoro-phenyl)-4-methyl-piperazine
• CAS: 218940-65-9
• 化学式: C₁₁H₁₅FN₂
• 分子量: 194.252
• InChiKey: UXUQHCICMDURET-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  6.5
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-bromomethyl-4-chloro-1-methyl-2-phenyl-1,2-dihydropyrazol-3-one 、 1-(2-fluorophenyl)-4-methylpiperazine 生成 4-Chloro-5-[4-(2-fluoro-phenyl)-piperazin-1-ylmethyl]-1-methyl-2-phenyl-1,2-dihydro-pyrazol-3-one
  参考文献：
  名称：

  Pyrazolone Compounds As Metabotropic Glutamate Receptor Agonists For The Treatment Of Neurological And Psychiatric Disorders

  摘要：

  公式（I）的化合物，其中R1，R2，R3，R4，R5，R6，X和n的定义如描述中的公式（I），制备该化合物的过程以及用于制备的新中间体，含有该化合物的制药组合物以及在治疗或预防与谷氨酸功能障碍有关的神经系统和精神障碍中使用该化合物。

  公开号：

  US20090069340A1
• 作为产物：
  描述：

  N-甲基哌嗪 、 1,2-二氟苯 在 potassium carbonate 作用下， 以 N-甲基吡咯烷酮 为溶剂， 反应 6.0h， 以85%的产率得到1-(2-fluorophenyl)-4-methylpiperazine
  参考文献：
  名称：

  Microwave-assisted amination from fluorobenzenes without catalyst and strong base

  摘要：

  A facile and versatile amination of fluorobenzenes has been developed in good to excellent yields under microwave irradiation in N-methylpyrrolidinone (NMP) without strong base and catalyst. The presence of additional halogen atom(s) enhanced the leaving ability of fluorine and meta fluorine gave higher activation than the ortho. It is remarkable that 1,2,3-trifluorobenzene, 1,2,4-trifluorobenzene and 1,2,4,5-tetrafluorobenzene can produce the regioselective mono-substituted products. (C) 2012 Elsevier B.V. All rights reserved.

  DOI：

  10.1016/j.jfluchem.2012.12.001

文献信息

• [EN] TRIAZACYCLODODECANSULFONAMIDE ("TCD")-BASED PROTEIN SECRETION INHIBITORS<br/>[FR] INHIBITEURS DE SÉCRÉTION DE PROTÉINE À BASE DE TRIAZACYCLODODÉCANSULFONAMIDE ("TCD")
  申请人：KEZAR LIFE SCIENCES

  公开号：WO2019178510A1

  公开（公告）日：2019-09-19

  Provided herein are triazacyclododecansulfonamide ("TCD")-based protein secretion inhibitors, such as inhibitors of Sec61, methods for their preparation, related pharmaceutical compositions, and methods for using the same. For example, provided herein are compounds of Formula (I) and pharmaceutically acceptable salts and compositions including the same. The compounds disclosed herein may be used, for example, in the treatment of diseases including inflammation and/or cancer.

  本文提供了基于三氮杂环十二烷磺酰胺（"TCD"）的蛋白质分泌抑制剂，例如Sec61的抑制剂，其制备方法，相关的药物组合物，以及使用它们的方法。例如，本文提供了符合Formula（I）的化合物及其药用盐和包括它们的组合物。本文披露的化合物可以用于治疗炎症和/或癌症等疾病。
• Novel Anthra [1, 2-d]imidazole-6,11-dione Derivatives, Preparation Method and application thereof
  申请人：HUANG Hsu-Shan

  公开号：US20110207719A1

  公开（公告）日：2011-08-25

  A series of novel anthra[1,2-d]imidazole-6,11-dione derivatives, and the preparation method and application of said derivatives, wherein said application includes a pharmaceutical composition containing said derivatives for treating cancer, and said application involves effects of said derivatives for inhibiting telomerase activity, inhibiting the growth of cancer cell, treating cancer and the like.

  一系列新型蒽[1,2-d]咪唑-6,11-二酮衍生物，以及所述衍生物的制备方法和应用，其中所述应用包括含有所述衍生物的用于治疗癌症的药物组合物，所述应用涉及所述衍生物抑制端粒酶活性、抑制癌细胞生长、治疗癌症等效果。
• Novel 1, 2-Disubstituted Amido-anthraquinone Derivatives, Preparation Method and application thereof
  申请人：HUANG Hsu-Shan

  公开号：US20110207739A1

  公开（公告）日：2011-08-25

  A series of novel 1,2-disubstituted amido-anthraquinone derivatives, and the preparation method and application of said derivatives. Said application includes said derivatives with therapeutically effective amount being prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.

  一系列新颖的1,2-二取代氨基蒽醌衍生物，以及所述衍生物的制备方法和应用。所述应用包括将所述衍生物与治疗有效量配制成药物组合物，用于抑制癌细胞生长，进一步治疗癌症。
• Gonadotropin Releasing Hormone Receptor Antagonist, Preparation Method Thereof And Pharmaceutical Composition Comprising The Same
  申请人：Kim Seon Mi

  公开号：US20130137661A1

  公开（公告）日：2013-05-30

  Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.

  披露了作为促性腺激素释放激素（“GnRH”）受体拮抗剂有用的化合物。
• NOVEL INDENO[1,2-c]QUINOLIN-11-ONE DERIVATIVES, PREPARATION METHOD AND APPLICATION THEREOF
  申请人：National Defense Medical Center

  公开号：US20150197492A1

  公开（公告）日：2015-07-16

  The present invention provides a novel series of indeno[1,2-c]quinolin-11-one derivatives and further provides their preparation methods as well as applications. Said applications includes utilizing such derivatives as pharmaceutical compositions for treating cancers; moreover, said applications includes the capability possessed by such derivatives to effectively inhibit cancer cell growth as well as the activity of Type I topoisomerases and can be further applied for cancer treatment.

  本发明提供了一系列新颖的indeno[1,2-c]quinolin-11-one衍生物，并进一步提供其制备方法以及应用。所述应用包括将这些衍生物用作治疗癌症的药物组合物；此外，所述应用包括这些衍生物具有有效抑制癌细胞生长以及抑制Ⅰ型拓扑异构酶活性的能力，并可进一步应用于癌症治疗。