4-甲基-2-乙酰氨基-5-氨基吡啶 | 475060-18-5

• 物质功能分类: 医药中间体 - 杂环化合物 - 吡啶类化合物
• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 4-甲基-2-乙酰氨基-5-氨基吡啶
• 中文别名: 2-乙酰氨基-5-氨基-4-甲基吡啶
• 英文名称: N1-(5-amino-4-methyl-pyridin-2-yl)acetamide
• 英文别名: N1-(5-amino-4-methyl-2-pyridyl)acetamide；N-(5-Amino-4-methylpyridin-2-yl)acetamide
• CAS: 475060-18-5
• 化学式: C₈H₁₁N₃O
• 分子量: 165.195
• InChiKey: IHZJIMFVFYNPMM-UHFFFAOYSA-N

物化性质

• 沸点：
  319.0±37.0 °C(Predicted)
• 密度：
  1.230±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  68
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-甲基-2-乙酰氨基-5-氨基吡啶 在 盐酸 、 tetrafluoroboric acid 、 sodium nitrite 作用下， 以 乙醇 、 甲苯 为溶剂， 生成 4-甲基-2-氨基-5-氟吡啶
  参考文献：
  名称：

  MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 4: Addressing the problem of poor stability due to photoisomerization of an acrylic acid moiety

  摘要：

  Exchange of the ethylene tether in a series of pyridopyrimidine-based MexAB-OprM specific efflux pump inhibitors to an amide bond stabilized the olefin of the acrylic acid moiety, preventing facile photoisomerization to the Z-isomer. Furthermore, the activity was drastically improved in the amide tether variants, providing extremely potent acrylic acid and vinyl tetrazole analogues. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.03.007
• 作为产物：
  描述：

  2-氨基-4-甲基-5-硝基吡啶 在 palladium on activated charcoal 氢气 作用下， 生成 4-甲基-2-乙酰氨基-5-氨基吡啶
  参考文献：
  名称：

  MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 4: Addressing the problem of poor stability due to photoisomerization of an acrylic acid moiety

  摘要：

  Exchange of the ethylene tether in a series of pyridopyrimidine-based MexAB-OprM specific efflux pump inhibitors to an amide bond stabilized the olefin of the acrylic acid moiety, preventing facile photoisomerization to the Z-isomer. Furthermore, the activity was drastically improved in the amide tether variants, providing extremely potent acrylic acid and vinyl tetrazole analogues. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.03.007

文献信息

• Drug efflux pump inhibitor
  申请人：DAIICHI PHARMACEUTICAL CO., LTD

  公开号：US20030092720A1

  公开（公告）日：2003-05-15

  A medicament for preventive and/or therapeutic treatment of a microbial infection which comprises as an active ingredient a compound represented by the following general formula (I): 1 wherein, R 1 and R 2 represent hydrogen atom, a halogen atom, hydroxyl group or the like, W 1 represents —CH═CH—, —CH 2 O—, —CH 2 CH 2 — or the like; R 3 represents hydrogen atom, a halogen atom, hydroxyl group or an amino group; R 4 represents hydrogen atom, a group of —OZ 0-4 R 5 (Z 0-4 represents an alkylene group, a fluorine-substituted alkylene group or a single bond, and R 5 represents a cyclic alkyl group, an aryl group or the like); W 2 represents a single bond or —C(R 8 )═C(R 9 )— (R 8 and R 9 represent hydrogen atom, a halogen atom, a lower alkyl group or the like, Q represents an acidic group, but W 2 and Q may together form vinylidenethiazolidinedione or an equivalent heterocyclic ring; m and n represent an integer of 0 to 2, and q represents an integer of 0 to 3.

  一种用于预防和/或治疗微生物感染的药物，其活性成分表示为以下一般式(I)的化合物： 其中，R1和R2代表氢原子、卤素原子、羟基或类似物，W1代表—CH═CH—、—CH2O—、—CH2CH2—或类似物；R3代表氢原子、卤素原子、羟基或氨基；R4代表氢原子、—OZ0-4R5（Z0-4代表烷基链、氟取代的烷基链或单键，R5代表环烷基、芳基或类似物）；W2代表单键或—C(R8)═C(R9)—（R8和R9代表氢原子、卤素原子、较低烷基或类似物，Q代表酸性基团，但W2和Q可以共同形成乙烯基噻唑二酮或等效的杂环环；m和n代表0到2的整数，q代表0到3的整数。
• Methods for treating retroviral infections
  申请人：Dunn Patrick James

  公开号：US20050239880A1

  公开（公告）日：2005-10-27

  The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according to formula I where Ar, R 1 -R 5 , R 11c and X 1 are as defined herein.

  本发明提供了用于治疗或预防HIV感染，治疗艾滋病或ARC的化合物，包括根据本文所定义的公式I给药的化合物，其中Ar、R1-R5、R11c和X1如本文所定义。
• Medicine for inhibiting drug elimination pump
  申请人：Nakayama Kiyoshi

  公开号：US20050009843A1

  公开（公告）日：2005-01-13

  A medicament for preventive and/or therapeutic treatment of a microbial infection which comprises as an active ingredient a compound represented by the following general formula (I): wherein, R 1 and R 2 represent hydrogen atom, a halogen atom, hydroxyl group or the like, W 1 represents —CH═CH—, —CH 2 O—, —CH 2 CH 2 — or the like; R 3 represents hydrogen atom, a halogen atom, hydroxyl group or an amino group; R 4 represents hydrogen atom, a group of —OZ 0-4 R 5 (Z 0-4 represents an alkylene group, a fluorine-substituted alkylene group or a single bond, and R 5 represents a cyclic alkyl group, an aryl group or the like); W 2 represents a single bond or —C(R 8 )═C(R 9 )—(R 8 and R 9 represent hydrogen atom, a halogen atom, a lower alkyl group or the like, Q represents an acidic group, but W 2 and Q may together form vinylidenethiazolidinedione or an equivalent heterocyclic ring; m and n represent an integer of 0 to 2, and q represents an integer of 0 to 3.

  预防和/或治疗微生物感染的药物，其活性成分为以下通用式（I）所表示的化合物：其中，R1和R2表示氢原子、卤原子、羟基或类似物，W1表示—CH═CH—、—CH2O—、—CH2CH2—或类似物；R3表示氢原子、卤原子、羟基或氨基；R4表示氢原子、—OZ0-4R5（Z0-4表示烷基、氟代烷基或单键，R5表示环烷基、芳基或类似物）；W2表示单键或—C（R8）═C（R9）—（R8和R9表示氢原子、卤原子、低烷基或类似物，Q表示酸性基团，但W2和Q可以共同形成乙烯基噻唑烷二酮或等效的杂环环；m和n表示0至2的整数，q表示0至3的整数。
• METHODS FOR TREATING RETROVIRAL INFECTIONS
  申请人：Dunn James Patrick

  公开号：US20100041648A1

  公开（公告）日：2010-02-18

  The present invention provides compositions for treating an HIV infection comprising administering a compound according to formula I where Ar, R 1 -R 5 , R 11c and X 1 are as defined herein with at least one carrier, excipient or diluent.

  本发明提供了用于治疗HIV感染的组合物，其包括按照式I给出的化合物与至少一种载体、赋形剂或稀释剂一起使用，其中Ar、R1-R5、R11c和X1的定义如本文所述。
• SUBSTITUTED AZOANTHRACENE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
  申请人：Mjalli Adnan M.M.

  公开号：US20110160198A1

  公开（公告）日：2011-06-30

  The present invention is directed to substituted azoanthracene derivatives or pharmaceutically acceptable salts thereof that modulate the human GLP-1 receptor and that may be useful in the treatment of diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial, such as diabetes mellitus type 2. The invention is also directed to pharmaceutical compositions comprising these compounds and to the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial.

  本发明涉及替代的偶氮蒽衍生物或其药学上可接受的盐，其调节人类GLP-1受体，并可用于治疗调节人类GLP-1受体有益的疾病、紊乱或病症，如2型糖尿病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗调节人类GLP-1受体有益的这些疾病、紊乱或病症中的使用。