6-甲氧基吡嗪-2-碳酰肼 | 59484-61-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 中文名称: 6-甲氧基吡嗪-2-碳酰肼
• 英文名称: 6-methoxypyrazine-2-carboxylic acid hydrazide
• 英文别名: 6-methoxypyrazine-2-carbohydrazide；6-methoxy-pyrazine-2-carboxylic acid hydrazide
• CAS: 59484-61-6
• 化学式: C₆H₈N₄O₂
• mdl: MFCD02258381
• 分子量: 168.155
• InChiKey: QVKCQQQKFUEWKG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.166
• 拓扑面积：
  90.1
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  6-甲氧基吡嗪-2-碳酰肼 以35%的产率得到
  参考文献：
  名称：

  RUDNICKA W.; FOKS H.; JANOWIEC M.; ZWOLSKA-KWIEK Z., ACTA POL. PHARM., 43,(1986) N 6, 523-528

  摘要：

  DOI：
• 作为产物：
  描述：

  6-氰基-2-氯吡嗪 在 一水合肼 作用下， 以 甲醇 、 乙醇 为溶剂， 反应 3.75h， 生成 6-甲氧基吡嗪-2-碳酰肼
  参考文献：
  名称：

  Studies on Pyrazine Derivatives. XLIX. Synthesis and Antibacterial Activity of 6-Methoxypyrazine-2-carboxylic Acid Hydrazide Derivatives

  摘要：

  The new 6-methoxy-pyrazine derivatives have been synthesized. 6-Methoxy-pyrazine-2-carboxylic acid hydrazide was used as an initial material to obtain mono- and dithioester of hydrazinecarbodithioic acid (2 and 3). Compound (2) in reaction with ethanolamine gave triazole derivative (8) with beta-hydoxyethyl substituent in 4-position and hydroxyl group in 6-position of pyrazine ring. Dithioester (3) in a reaction with morpholine cyclized to 1,3,4-oxadiazole (11). The same substrate with alkyldiamines gave the few following derivatives: 1,3-diazacycloalkane derivatives (9 and 10), S-methyl-1,3,4-oxadiazole derivative (12) and 1,2,4-triazoletetrahydropyrimidine (13). The compounds obtained were tested in vitro for their activity towards pathogenic strains of anaerobic and aerobic bacteria. Derivative (9) was the most active against both types of tested strains.

  DOI：

  10.3987/com-06-10867

文献信息

• Heteroaryl-substituted triazoles as APJ receptor agonists
  申请人：AMGEN INC.

  公开号：US11046680B1

  公开（公告）日：2021-06-29

  Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.

  式（I）和式（II）化合物、其药学上可接受的盐、前述任何化合物的立体异构体或其混合物是 APJ 受体的激动剂，可用于治疗心血管疾病和其他疾病。式 I 和式 II 的化合物具有如下结构： 其中变量的定义在本文中提供。
• PANCECHOWSKA-KSEPKO, DANUTA;FOKS, HENRYK;JANOWIEC, MIECZYSLAW;ZWOLSKA-KWI+, ACTA POL. PHARM. , 45,(1988) N, C. 373-379
  作者：PANCECHOWSKA-KSEPKO, DANUTA、FOKS, HENRYK、JANOWIEC, MIECZYSLAW、ZWOLSKA-KWI+

  DOI：——

  日期：——
• HETEROARYL-SUBSTITUTED TRIAZOLES AS APJ RECEPTOR AGONISTS
  申请人：Amgen Inc.

  公开号：EP3541805B1

  公开（公告）日：2020-10-14