6-Hydroxy-pyridine-2-carboxylic acid tert-butylamide | 1033809-08-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 6-Hydroxy-pyridine-2-carboxylic acid tert-butylamide
• 英文别名: N-tert-butyl-6-oxo-1H-pyridine-2-carboxamide
• CAS: 1033809-08-3
• 化学式: C₁₀H₁₄N₂O₂
• 分子量: 194.233
• InChiKey: KZYZHNQVBHHRHM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  58.2
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  甲基磺酰氯 、 6-Hydroxy-pyridine-2-carboxylic acid tert-butylamide 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 Methanesulfonic acid 6-tert-butylcarbamoyl-pyridin-2-yl ester
  参考文献：
  名称：

  Synthesis and Insecticidal Activity of Novel Pyridine Methanesulfonates

  摘要：

  A model has been developed which has led to the design and synthesis of novel 6-methanesulfonyloxypyridine-2-carboxamides with insecticidal activity, low mammalian toxicity and safety to aquatic organisms. The amides formed from amines with alpha branching (e.g. isopropyl and sec-butyl) demonstrated the highest level of activity. Rice nursery box field test results on laboratory raised insects gave insufficient control of the entire Japanese hopper spectrum to warrant further development of these compounds.

  DOI：

  10.1002/(sici)1096-9063(199708)50:4<319::aid-ps595>3.0.co;2-e
• 作为产物：
  描述：

  6-羟基吡啶-2-羧酸 以 四氢呋喃 为溶剂， 反应 1.5h， 生成 6-Hydroxy-pyridine-2-carboxylic acid tert-butylamide
  参考文献：
  名称：

  Synthesis and Insecticidal Activity of Novel Pyridine Methanesulfonates

  摘要：

  A model has been developed which has led to the design and synthesis of novel 6-methanesulfonyloxypyridine-2-carboxamides with insecticidal activity, low mammalian toxicity and safety to aquatic organisms. The amides formed from amines with alpha branching (e.g. isopropyl and sec-butyl) demonstrated the highest level of activity. Rice nursery box field test results on laboratory raised insects gave insufficient control of the entire Japanese hopper spectrum to warrant further development of these compounds.

  DOI：

  10.1002/(sici)1096-9063(199708)50:4<319::aid-ps595>3.0.co;2-e

文献信息

• Bridged bicyclic inhibitors of menin-MLL and methods of use
  申请人：Kura Oncology, Inc.

  公开号：US10752639B2

  公开（公告）日：2020-08-25

  The present disclosure provides compounds of Formula (I-E) for inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The compounds are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.

  本公开提供了式 (I-E) 的化合物，用于抑制 menin 与 MLL1、MLL2 和 MLL 融合肿瘤蛋白的相互作用。这些化合物可用于治疗白血病、实体癌、糖尿病和其他依赖于 MLL1、MLL2、MLL 融合蛋白和/或 menin 活性的疾病。
• BRIDGED BICYCLIC INHIBITORS OF MENIN-MLL AND METHODS OF USE
  申请人：Kura Oncology, Inc.

  公开号：US20210107917A1

  公开（公告）日：2021-04-15

  The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. Compositions for use in these methods are also provided.
• Synthesis and Insecticidal Activity of Novel Pyridine Methanesulfonates
  作者：Bruce L. Finkelstein、Melissa A. Martz、Christopher J. Strock

  DOI：10.1002/(sici)1096-9063(199708)50:4<319::aid-ps595>3.0.co;2-e

  日期：1997.8

  A model has been developed which has led to the design and synthesis of novel 6-methanesulfonyloxypyridine-2-carboxamides with insecticidal activity, low mammalian toxicity and safety to aquatic organisms. The amides formed from amines with alpha branching (e.g. isopropyl and sec-butyl) demonstrated the highest level of activity. Rice nursery box field test results on laboratory raised insects gave insufficient control of the entire Japanese hopper spectrum to warrant further development of these compounds.