N-formyl-2-quinolylamine | 89067-40-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: N-formyl-2-quinolylamine
• 英文别名: N-Quinolin-2-ylformamide
• CAS: 89067-40-3
• 化学式: C₁₀H₈N₂O
• 分子量: 172.186
• InChiKey: RNKXGTCTNKXYFB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  42
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  2-喹啉甲酸甲酯 在 羟胺 、 sodium methylate 作用下， 以 甲醇 为溶剂， 反应 48.0h， 生成 N-formyl-2-quinolylamine
  参考文献：
  名称：

  Pajak, Janina; Lipczynska-Kochany, Ewa; Eckstein, Zygmunt, Polish Journal of Chemistry, 1982, vol. 56, # 3, p. 593 - 599

  摘要：

  DOI：

文献信息

• Tyrosine phosphatase inhibitors
  申请人：——

  公开号：US20030144338A1

  公开（公告）日：2003-07-31

  A compound of the formula (I): 1 wherein X 1 and X 2 are the same or different and each is a bond or a spacer having 1 to 20 atom(s) in the main chain; one of R 1 and R 2 is a cycle group having substituent(s) selected from 1) an optionally substituted carboxy-C 1-6 alkoxy group and 2) an optionally substituted carboxy-C 1-6 aliphatic hydrocarbon group, wherein the cycle group optionally has additional substituent(s), and the other is an optionally substituted cycle group or a hydrogen atom; and R 3 , R 4 and R 5 are the same or different and each is a hydrogen atom or a substituent, or R 4 may link together with R 3 or R 5 to form an optionally substituted ring; provided that when R 3 is a hydrogen atom, R 4 is a hydrogen atom and R 5 is methyl, X 2 —R 2 is not 4-cyclohexylphenyl; when R 3 is 4-methoxyphenyl, R 4 is a hydrogen atom and R 5 is methyl, X 2 —R 2 is not 4-methoxyphenyl; and when R 1 or R 2 is a hydrogen atom, the adjacent X 1 or X 2 is not a C 1-7 alkylene; or a salt thereof exhibits a protein tyrosine phosphatase inhibitory action and is useful as a prophylactic or therapeutic agent for diabetes or the like.

  式（I）的化合物： 其中X1和X2相同或不同，每个都是主链中具有1至20个原子的键或间隔物； R1和R2中的一个是具有取代基的环基，所述取代基选自1）可选择地取代的羧基-C1-6烷氧基和2）可选择地取代的羧基-C1-6脂肪烃基，其中所述环基可选择地具有额外的取代基，另一个是可选择地取代的环基或氢原子；以及 R3、R4和R5相同或不同，每个是氢原子或取代基，或R4可以与R3或R5结合形成可选择地取代的环； 但是当R3是氢原子时，R4是氢原子且R5是甲基时，X2—R2不是4-环己基苯基；当R3是4-甲氧基苯基，R4是氢原子且R5是甲基时，X2—R2不是4-甲氧基苯基；当R1或R2是氢原子时，相邻的X1或X2不是C1-7烷基； 或其盐具有蛋白酪氨酸磷酸酶抑制作用，并且可用作糖尿病等疾病的预防或治疗剂。
• Melanin-concentrating hormone antagonist
  申请人：——

  公开号：US20030158177A1

  公开（公告）日：2003-08-21

  A melanin-concentrating hormone antagonist comprising a compound of the formula: 1 wherein R is hydrogen atom or a cyclic group which may be substituted; X is a bond or a spacer having a main chain of 1 to 10 atoms; Y is a spacer having a main chain of 1 to 6 atoms; ring A is benzene ring which may be further substituted; ring B is a 5- to 9-membered nitrogen-containing non-aromatic heterocyclic ring which may be further substituted; R 1 and R 2 are the same or different and are hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; or R 1 and R 2 , together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic ring which may be substituted; or R 2 , together with the adjacent nitrogen atom and Y, may form a nitrogen-containing heterocyclic ring which may be substituted; or a salt thereof is useful as a preventive or therapeutic agent for obesity, etc.

  一种黑素浓缩激素拮抗剂，包括以下结构的化合物：其中R是氢原子或可能被取代的环状基团；X是具有1到10个原子主链的键或间隔物；Y是具有1到6个原子主链的间隔物；环A是苯环，可能进一步被取代；环B是一个含氮的非芳香杂环环，成员数为5到9，可能进一步被取代；R1和R2相同或不同，是氢原子、可能被取代的烃基或可能被取代的杂环基；或者R1和R2，与相邻的氮原子一起，可以形成一个可能被取代的含氮杂环环；或者R2，与相邻的氮原子和Y一起，可以形成一个可能被取代的含氮杂环环；或其盐可用作肥胖等疾病的预防或治疗剂。
• Epoxycarboxamide compound, azide compound, and amino alcohol compound, and process for preparing alpha-keto amide compound using them
  申请人：Seikagaku Corporation

  公开号：US20030153788A1

  公开（公告）日：2003-08-14

  The present invention is to provide manufacturing intermediates which can be led to useful &agr;-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide epoxycarboxamide compounds, azide compounds and amino alcohol compounds represented by the following formulae: 1 wherein R 1 and R 2 each represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R 3 represents alkyl group, alkenyl group, aromatic hydrocarbon group, heterocyclic group, R 6 —O— or R 7 —N(R 8 )—; where R 6 represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R 7 and R 8 each represents hydrogen atom, alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group, and, R 4 and R 5 represent the same groups as R 7 and R 8 , respectively, and R 4 and R 5 optionally form a ring together; and X represents —O— or —N(R 9 )—, where R 9 represents hydrogen atom or alkyl group, and X optionally forms a ring together with R 4 or R 5 , and processes for preparing &agr;-keto amide compound using the same.

  本发明旨在提供制造中间体，以极其经济和立体选择性地导向有蛋白酶抑制活性的有用α-酮酰胺化合物，并提供由以下式表示的环氧羧酰胺化合物，叠氮化合物和氨基醇化合物：其中R1和R2分别表示烷基，烯基，芳香族烃基或杂环基；R3表示烷基，烯基，芳香族烃基，杂环基，R6-O-或R7-N（R8）-；其中R6表示烷基，烯基，芳香族烃基或杂环基；R7和R8分别表示氢原子，烷基，烯基，芳香族烃基或杂环基，而R4和R5分别表示与R7和R8相同的基团，R4和R5可选择性地共同形成环；X表示-O-或-N（R9）-，其中R9表示氢原子或烷基，X可选择性地与R4或R5共同形成环，以及使用它们制备α-酮酰胺化合物的方法。
• Compounds for inhibiting KSP kinesin activity
  申请人：Tagat R. Jayaram

  公开号：US20060247320A1

  公开（公告）日：2006-11-02

  The present invention provides compounds of Formula I (wherein R 1 , R 3 , X, W, Z and ring Y are as defined herein). The present invention also provides compositions comprising these compounds that are useful for treating cellular proliferative diseases or disorders associated with KSP kinesin activity and for inhibiting KSP kinesin activity.

  本发明提供了I式化合物（其中R1、R3、X、W、Z和环Y的定义如本文所述）。本发明还提供了包含这些化合物的组合物，用于治疗与KSP肌动蛋白活性相关的细胞增殖性疾病或紊乱，并抑制KSP肌动蛋白活性。
• Aza-Substituted Spiro Derivatives
  申请人：Jitsuoka Makoto

  公开号：US20090258871A1

  公开（公告）日：2009-10-15

  A compound of the following formula (I) or its pharmaceutically-acceptable salt is provided: [wherein X, Y, Z and W each independently represent a methine group or a nitrogen atom, provided that a case where all of X, Y, Z and W are methine group; A represents —O— or the like, B represents —C(O)— or the like, D represent —(CH 2 )m 2 -, —O— or the like, and m2 represents 0 or 1; Q represents a methine group or a nitrogen atom; and R represents a group represented by the following formula (II-1) (wherein R 6 , R 7 and R 8 independently represent a lower alkyl group or the like].

  提供以下式子（I）的化合物或其药学上可接受的盐：[其中X、Y、Z和W各自独立地表示甲基基团或氮原子，前提是当X、Y、Z和W全部为甲基基团时；A表示—O—或类似物，B表示—C（O）—或类似物，D表示—（CH2）m2-、—O—或类似物，m2表示0或1；Q表示甲基基团或氮原子；R表示由以下式子（II-1）表示的基团（其中R6、R7和R8各自独立地表示较低的烷基基团或类似物）。