1-(6-bromopyridin-2-yl)piperidin-2-one | 1027512-06-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 1-(6-bromopyridin-2-yl)piperidin-2-one
• CAS: 1027512-06-6
• 化学式: C₁₀H₁₁BrN₂O
• 分子量: 255.114
• InChiKey: KAPHLBDJDWTCRK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  33.2
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(6-bromopyridin-2-yl)piperidin-2-one 、 6-(2-amino-4-methyl-1,3-thiazol-5-yl)-2-[(1S)-1-cyclopropylethyl]-N-methyl-3-oxo-2,3-dihydro-1H-isoindole-4-sulfonamide 在 second generation XantPhos catalyst 、 sodium carbonate 、 4,5-双二苯基膦-9,9-二甲基氧杂蒽 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 1.0h， 生成 2-[(1S)-1-cyclopropylethyl]-N-methyl-6-(4-methyl-2-{[6-(2-oxopiperidin-1-yl)pyridin-2-yl]amino}-1,3-thiazol-5-yl)-3-oxo-2,3-dihydro-1H-isoindole-4-sulfonamide
  参考文献：
  名称：

  Discovery of AZD8154, a Dual PI3Kγδ Inhibitor for the Treatment of Asthma

  摘要：

  DOI：

  10.1021/acs.jmedchem.1c00434
• 作为产物：
  描述：

  2-氨基-6-溴吡啶 在 吡啶 、 caesium carbonate 作用下， 以 N,N-二甲基甲酰胺 、 乙腈 为溶剂， 反应 7.0h， 生成 1-(6-bromopyridin-2-yl)piperidin-2-one
  参考文献：
  名称：

  Discovery of AZD8154, a Dual PI3Kγδ Inhibitor for the Treatment of Asthma

  摘要：

  DOI：

  10.1021/acs.jmedchem.1c00434

文献信息

• [EN] 5-[2-(PYRIDIN-2-YLAMINO)-1,3-THIAZOL-5-YL]-2,3-DIHYDRO-1 H-ISOINDOL-1 -ONE DERIVATIVES AND THEIR USE AS DUAL INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE DELTA & GAMMA<br/>[FR] DÉRIVÉS DE 5-[2-(PYRIDIN-2-YLAMINO)-1,3-THIAZOL-5-YL]-2,3-DIHYDRO-1 H-ISOINDOL-1 -ONE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DOUBLES DE PHOSPHATIDYLINOSITOL 3-KINASE DELTA & GAMMA
  申请人：ASTRAZENECA AB

  公开号：WO2018055040A1

  公开（公告）日：2018-03-29

  There are disclosed certain novel compounds (including pharmaceutically acceptable salts thereof) (I) that inhibit phosphatidylinositol 3-kinase gamma (PI3Kδ) and phosphatidylinositol 3-kinase gamma (ΡΙ3Κγ) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

  披露了一些新颖的化合物（包括其药用盐）（I），这些化合物抑制磷脂酰肌醇3-激酶γ（PI3Kδ）和磷脂酰肌醇3-激酶γ（ΡΙ3Κγ）的活性，用于治疗和/或预防包括哮喘和慢性阻塞性肺部疾病（COPD）在内的临床疾病，用于治疗，包含它们的药物组合物以及制备这些化合物的方法。
• (S)-2-(1-cyclopropylethyl)-5-(4-methyl-2-((6-(2-oxopyrrolidin-1-yl)pyridin-2-yl)amino) thiazol-5-yl)-7-(methylsulfonyl)isoindolin-1-one as a phosphatidylinositol 3-kinase inhibitor
  申请人：AstraZeneca AB

  公开号：US10961236B2

  公开（公告）日：2021-03-30

  Disclosed herein is the compound (S)-2-(1-cyclopropylethyl)-5-(4-methyl-2-((6-(2-oxopyrrolidin-1-yl)pyridin-2-yl)amino)thiazol-5-yl)-7-(methylsulfonyl)isoindolin-1-one of the following structure: and/or pharmaceutically acceptable salts and/or pharmaceutical compositions thereof, which inhibit phosphatidylinositol 3-kinase (PI3K) activity.

  本发明公开了以下结构的化合物(S)-2-(1-环丙基乙基)-5-(4-甲基-2-((6-(2-氧代吡咯烷-1-基)吡啶-2-基)氨基)噻唑-5-基)-7-(甲磺酰基)异吲哚啉-1-酮： 和/或其药学上可接受的盐和/或药物组合物，可抑制磷脂酰肌醇 3- 激酶 (PI3K) 的活性。
• 5-[2-(PYRIDIN-2-YLAMINO)-1,3-THIAZOL-5-YL]-2,3-DIHYDRO-1 H-ISOINDOL-1 -ONE DERIVATIVES AND THEIR USE AS DUAL INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE DELTA&GAMMA
  申请人：Astrazeneca AB

  公开号：EP3515910A1

  公开（公告）日：2019-07-31
• 5-[2-(PYRIDIN-2-YLAMINO)-1,3-THIAZOL-5-YL]-2,3-DIHYDRO-1H-ISOINDOL-1-ONE DERIVATIVES AND THEIR USE AS DUAL INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE DELTA & GAMMA
  申请人：Astrazeneca AB

  公开号：EP3515910B1

  公开（公告）日：2020-07-15
• 5-[2-(PYRIDIN-2-YLAMINO)-1,3-THIAZOL-5-YL]-2,3-DIHYDRO-1 H-ISOINDOL-1 -ONE DERIVATIVES AND THEIR USE AS DUAL INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE DELTA & GAMMA
  申请人：AstraZeneca AB

  公开号：US20200308164A1

  公开（公告）日：2020-10-01

  There are disclosed certain novel compounds (including pharmaceutically acceptable salts thereof), that inhibit phosphatidylinositol 3-kinase gamma (PI3Kγ) and phosphatidylinositol 3-kinase gamma (PI3Kγ) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.