tert-butyl (2-aminopyrimidin-5-yl)acetate | 1443739-40-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: tert-butyl (2-aminopyrimidin-5-yl)acetate
• 英文别名: Tert-butyl (2-aminopyrimidin-5-yl)acetate；tert-butyl 2-(2-aminopyrimidin-5-yl)acetate
• CAS: 1443739-40-9
• 化学式: C₁₀H₁₅N₃O₂
• 分子量: 209.248
• InChiKey: NSCSKYIITJCZMU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  78.1
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  tert-butyl (2-aminopyrimidin-5-yl)acetate 在 溶剂黄146 、 三氟乙酸 作用下， 以 四氢呋喃 、 甲醇 、 二氯甲烷 为溶剂， 反应 0.17h， 生成 [2-({2-[(1S,2S)-2-{1-[(benzyloxy)carbonyl]piperidin-4-yl}cyclopropyl]ethyl}amino)pyrimidin-5-yl]acetic acid
  参考文献：
  名称：

  [EN] SUBSTITUTED CYCLOPROPYL COMPOUNDS USEFUL AS GPR119 AGONISTS
  [FR] COMPOSÉS CYCLOPROPYLÉS SUBSTITUÉS UTILES COMME AGONISTES DE GPR119

  摘要：

  公开了公式I的环丙基化合物及其药用盐，用于治疗或预防2型糖尿病和类似疾病。这些化合物可作为G蛋白偶联受体GPR-119的激动剂。还包括药物组合物和治疗方法。

  公开号：

  WO2013122821A1
• 作为产物：
  描述：

  溴乙酸叔丁酯 在 tris-(dibenzylideneacetone)dipalladium(0) 、 三甲基氯硅烷 、 2-二环己基磷-2,4,6-三异丙基联苯 作用下， 以 四氢呋喃 为溶剂， 反应 5.0h， 生成 tert-butyl (2-aminopyrimidin-5-yl)acetate
  参考文献：
  名称：

  [EN] BICYCLIC PHTHALAZIN-1(2H)-ONE DERIVATIVES AND RELATED USES
  [FR] DÉRIVÉS BICYCLIQUES DE PHTALAZIN-1(2H)-ONE ET UTILISATIONS ASSOCIÉES

  摘要：

  The present disclosure relates to compounds of Formula (III): and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.

  公开号：

  WO2023133271A1

文献信息

• INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
  申请人：MERCK SHARP & DOHME CORP.

  公开号：US20140336177A1

  公开（公告）日：2014-11-13

  The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.

  本发明提供了I式化合物及其药学上可接受的盐，其是ROMK（Kir1.1）通道的抑制剂。这些化合物作为利尿剂和钠利尿剂，是治疗和预防包括高血压和由过度盐和水潴留引起的疾病等医学状况的有价值的药学活性化合物。
• Inhibitors of the renal outer medullary potassium channel
  申请人：Pio Barbara

  公开号：US09206199B2

  公开（公告）日：2015-12-08

  The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.

  本发明提供了I式化合物及其药学上可接受的盐，该化合物是ROMK(Kir1.1)通道的抑制剂。该化合物具有利尿和排钠作用，是治疗和预防包括高血压和由过多盐和水潴留引起的医疗状况的有价值的药物活性化合物。
• [EN] SUBSTITUTED CYCLOPROPYL COMPOUNDS USEFUL AS GPR119 AGONISTS<br/>[FR] COMPOSÉS CYCLOPROPYLÉS SUBSTITUÉS UTILES COMME AGONISTES DE GPR119
  申请人：MERCK SHARP & DOHME

  公开号：WO2013122821A1

  公开（公告）日：2013-08-22

  Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.

  公开了公式I的环丙基化合物及其药用盐，用于治疗或预防2型糖尿病和类似疾病。这些化合物可作为G蛋白偶联受体GPR-119的激动剂。还包括药物组合物和治疗方法。
• [EN] BICYCLIC PHTHALAZIN-1(2H)-ONE DERIVATIVES AND RELATED USES<br/>[FR] DÉRIVÉS BICYCLIQUES DE PHTALAZIN-1(2H)-ONE ET UTILISATIONS ASSOCIÉES
  申请人：[en]NODTHERA LIMITED

  公开号：WO2023133271A1

  公开（公告）日：2023-07-13

  The present disclosure relates to compounds of Formula (III): and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.