4,6-dichloro-N-(prop-2-yn-1-yl)pyrimidine-5-carboxamide | 285991-69-7

• 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: 4,6-dichloro-N-(prop-2-yn-1-yl)pyrimidine-5-carboxamide
• 英文别名: 4,6-dichloro-N-prop-2-ynylpyrimidine-5-carboxamide
• CAS: 285991-69-7
• 化学式: C₈H₅Cl₂N₃O
• 分子量: 230.053
• InChiKey: CWYIPAQVCCHPJA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  54.9
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4,6-dichloro-N-(prop-2-yn-1-yl)pyrimidine-5-carboxamide 以 硝基苯 为溶剂， 以37 %的产率得到4-氯-1H-吡咯并[3,4-c]吡啶-3(2H)-酮
  参考文献：
  名称：

  [EN] COMPOUNDS FOR USE IN TREATING NEUROLOGICAL DISORDERS
  [FR] COMPOSÉS DESTINÉS À ÊTRE UTILISÉS DANS LE TRAITEMENT DE TROUBLES NEUROLOGIQUES

  摘要：

  This disclosure provides compounds of formula (I) and pharmaceutically acceptable salts thereof, that inhibit Dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A). These chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) DYRK1A activation contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., a neurological disorder) in a subject (e.g., a human). This disclosure also provides compositions containing the same as well as methods of using and making the same.

  公开号：

  WO2023107722A1
• 作为产物：
  描述：

  4,6-二氯-5-嘧啶甲醛 在 磺酰氯 、 三乙胺 作用下， 生成 4,6-dichloro-N-(prop-2-yn-1-yl)pyrimidine-5-carboxamide
  参考文献：
  名称：

  Tarasov, Evgeniy V.; Henckens, Anja; Ceulemans, Erik, Synlett, 2000, # 5, p. 625 - 626

  摘要：

  DOI：

文献信息

• [EN] 2-CYANOISOINDOLINE DERIVATIVES FOR TREATING CANCER<br/>[FR] DÉRIVÉS DE 2-CYANOISOINDOLINE POUR LE TRAITEMENT DU CANCER
  申请人：MISSION THERAPEUTICS LTD

  公开号：WO2017158388A1

  公开（公告）日：2017-09-21

  The invention relates to novel compounds of formula I which are inhibitors of deubiquitylating enzymes (DUBs) and/or desumoylating enzymes. In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 7 or ubiquitin specific peptidase 7 (USP7). The invention further relates to methods for the preparation of these compounds and to their use in the treatment of cancer.

  这项发明涉及公式I的新化合物，这些化合物是去泛素化酶（DUBs）和/或去泛素化酶的抑制剂。具体来说，该发明涉及抑制泛素C端水解酶7或泛素特异性肽酶7（USP7）。该发明还涉及这些化合物的制备方法以及它们在癌症治疗中的应用。
• Synthesis of fused bicyclic pyridines with microwave-assisted intramolecular hetero-Diels–Alder cycloaddition of acetylenic pyrimidines
  作者：Bin Shao

  DOI：10.1016/j.tetlet.2005.03.098

  日期：2005.5

  to microwave irradiation. In contrast to conventional heating, the microwave irradiations generally gave clean conversion to fused bicyclic pyridines for all substrates reported with shorter reaction time. This method has been successfully applied to the synthesis of both fused lactones and lactams.

  合成了一系列炔属嘧啶并对其进行微波辐射。与常规加热相比，对于所有报道的反应时间较短的底物，微波辐射通常都能将其干净地转化为稠合的双环吡啶。该方法已经成功地应用于融合的内酯和内酰胺的合成。
• 2-cyanoisoindoline derivatives for treating cancer
  申请人：MISSION THERAPEUTICS LIMITED

  公开号：US10683269B2

  公开（公告）日：2020-06-16

  The invention relates to novel compounds of formula I which are inhibitors of deubiquitylating enzymes (DUBs) and/or desumoylating enzymes. In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 7 or ubiquitin specific peptidase 7 (USP7). The invention further relates to methods for the preparation of these compounds and to their use in the treatment of cancer.

  本发明涉及式 I 的新型化合物，它们是去泛素化酶 (DUB) 和/或去umoylating 酶的抑制剂。特别是，本发明涉及对泛素 C 端水解酶 7 或泛素特异性肽酶 7（USP7）的抑制。本发明还涉及这些化合物的制备方法及其在治疗癌症中的用途。
• [EN] THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN<br/>[FR] AGENTS THERAPEUTIQUES POUR TRAITEMENT DE LA DOULEUR
  申请人：EURO CELTIQUE SA

  公开号：WO2005056524A3

  公开（公告）日：2005-09-22
• 2-CYANOISOINDOLINE DERIVATIVES FOR TREATING CANCER
  申请人：Mission Therapeutics Limited

  公开号：EP3429994A1

  公开（公告）日：2019-01-23