N-乙基-3,5-二氟苯胺 | 119284-23-0

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: N-乙基-3,5-二氟苯胺
• 英文名称: N-ethyl-3,5-difluoroaniline
• CAS: 119284-23-0
• 化学式: C₈H₉F₂N
• mdl: MFCD09859812
• 分子量: 157.163
• InChiKey: BNBCNJSNRMAIGH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  12
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2921420090

反应信息

• 作为反应物：
  描述：

  N-乙基-3,5-二氟苯胺 在 palladium on activated charcoal 氢气 作用下， 以 乙醇 为溶剂， 生成 1-(3,5-Dimethoxy-phenyl)-7-hydroxy-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid (3,5-difluoro-phenyl)-ethyl-amide
  参考文献：
  名称：

  A novel class of apical sodium-dependent bile acid transporter inhibitors: the amphiphilic 4-oxo-1-phenyl-1,4-dihydroquinoline derivatives

  摘要：

  A series of 4-oxo-1-phenyl-1,4-dihydroquinolines possessing a linker and an ammonio moiety were synthesized and found to inhibit the apical sodium-dependent bile acid transporter (ASBT). The potency of ASBT inhibition varied with the position and length of the linking tether. Compound 21e effectively lowered the total serum cholesterol levels in hamsters. (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2003.12.063

文献信息

• [EN] QUINOXALINE AND PYRIDOPYRAZINE DERIVATIVES AS PI3KBETA INHIBITORS<br/>[FR] DÉRIVÉS DE QUINOXALINE ET DE PYRIDOPYRAZINE À TITRE D'INHIBITEURS DE PI3KΒ
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2017060406A1

  公开（公告）日：2017-04-13

  The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3Kβ inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

  本发明涉及式（I）所示的取代喹喹啉和吡啶吡嘧啶衍生物，其中变量的含义如权利要求中所定义。根据本发明的化合物可用作pI3Kβ抑制剂。本发明还涉及含有上述化合物作为活性成分的药物组合物，以及将上述化合物用作药物的用途。
• [EN] OPTICALLY ACTIVE 1-(FLUORO-,TRIFLUOROMETHYL-OR TRIFLUOROMETHOXY-SUBSTITUTED PHENYL)ALKYLAMINE N-MONOALKYL DERIVATIVES AND PROCESS FOR PRODUCING SAME<br/>[FR] DERIVES DE 1-( PHENYLE A SUBSTITUTION FLUORO,TRIFLUOROMETHYLE OU TRIFLUOROMETHOXY)ALKYLAMINE N-MONOALKYLE OPTIQUEMENT ACTIFS ET LEUR PROCEDE DE PRODUCTION
  申请人：CENTRAL GLASS CO LTD

  公开号：WO2004022521A1

  公开（公告）日：2004-03-18

  An optically active 1-(fluoro-, trifluoromethyl- or trifluoromethoxy-substituted phenyl)alkylamine N-monoalkyl derivative represented by the formula [4] is produced by a process including (a) reacting an optically active secondary amine, represented by the formula [1], with an alkylation agent R2-X, in the presence of a base, thereby converting the secondary amine into an optically active tertiary amine represented by the formula [3]; and (b) subjecting the tertiary amine to a hydrogenolysis, thereby producing the N-monoalkyl derivative,wherein R represents a fluorine atom, trifluoromethyl group or trifluoromethoxy group, n represents an integer of from 1 to 5, each of R1 and R2 independently represents an alkyl group having a carbon atom number of from 1 to 6, Me represents a methyl group, Ar represents a phenyl group or 1- or 2-naphthyl group, * represents a chiral carbon, and X represents a leaving group.

  通过以下过程制备一种光学活性的1-(氟代、三氟甲基或三氟甲氧基取代的苯基)烷基胺N-单烷基衍生物，其化学式如下[4]：(a) 用碱存在下，将光学活性的二级胺（化学式[1]表示）与烷基化剂R2-X反应，从而将二级胺转化为光学活性的三级胺（化学式[3]表示）；(b) 将三级胺进行氢解作用，从而生成N-单烷基衍生物，其中R代表氟原子、三氟甲基基团或三氟甲氧基团，n代表1至5之间的整数，R1和R2分别代表具有1至6个碳原子的烷基基团，Me代表甲基基团，Ar代表苯基或1-或2-萘基，*代表一个手性碳，X代表一个离去基团。
• Metabotropic glutamate receptor antagonists and their use for treating central nervous system diseases
  申请人：NPS PHARMACEUTICALS, INC.

  公开号：US20030013715A1

  公开（公告）日：2003-01-16

  The present invention provides compounds, and pharmaceutical compositions containing those compounds, that are active at metabotropic glutamate receptors. The compounds are useful for treating neurological diseases and disorders. Methods of preparing the compounds also are disclosed.

  本发明提供了一种在代谢型谷氨酸受体上具有活性的化合物和含有这些化合物的药物组合物，这些化合物对治疗神经系统疾病和紊乱有用。本发明还公开了制备这些化合物的方法。
• PYRROLOTRIAZINE COMPOUNDS AS KINASE INHIBITORS
  申请人：Fink Brian E.

  公开号：US20090048244A1

  公开（公告）日：2009-02-19

  The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.

  本发明提供公式I化合物及其药学上可接受的盐。公式I化合物抑制生长因子受体的酪氨酸激酶活性，如HER1、HER2和HER4，因此使它们有用作抗增殖剂。公式I化合物也适用于治疗与通过生长因子受体进行信号转导途径相关的其他疾病。
• Titanocene, deren Verwendung und N-substituierte Fluoraniline
  申请人：CIBA-GEIGY AG

  公开号：EP0318893A2

  公开（公告）日：1989-06-07

  Titanocene mit zwei 5-gliedrigen Cyclodienylgruppen, z.B. Cyclopentadienyl, und ein oder zwei 6-gliedrigen carbocyclischen oder 5-oder 6-gliedrigen heterocyclischen aromatischen Ringen, die in mindestens einer der beiden Orthostellungen zur Titankohlenstoffbindung mit einem Fluoratom substituiert sind und als weiteren Substituenten einen substituierten Aminorest enthalten, eignen sich als Photoinitiatoren für die strahlungsinduzierte Polymerisation von ethylenisch ungesättigten Verbindungen.

  具有两个 5 元环二烯基（如环戊二烯基）和一个或两个 6 元碳环或 5 元或 6 元杂环芳香环的二茂钛，在钛-碳键的两个正交位置中至少有一个位置被氟原子取代，并含有一个取代氨基作为进一步取代基，适合用作乙烯不饱和化合物辐射诱导聚合的光引发剂。