4-(Bromomethyl)-2-(difluoromethoxy)pyridine | 1268517-84-5

• 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: 4-(Bromomethyl)-2-(difluoromethoxy)pyridine
• CAS: 1268517-84-5
• 化学式: C₇H₆BrF₂NO
• 分子量: 238.03
• InChiKey: HXWAYWSNGXCTEO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  22.1
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-(2,6-Dimethoxyphenyl)-3-methylpyrrolidin-2-one 、 4-(Bromomethyl)-2-(difluoromethoxy)pyridine 生成 1-((2-(Difluoromethoxy)pyridin-4-yl)methyl)-5-(2,6-dimethoxyphenyl)-3-methylpyrrolidin-2-one
  参考文献：
  名称：

  Lactam derivatives useful as orexin receptor antagonists

  摘要：

  本发明涉及公式(I)的内酰胺衍生物，其中Y，R1，R2和R3如描述中所述，它们的制备，其药学上可接受的盐以及它们作为药物的用途，含有一个或多个公式（I）化合物的药物组合物，特别是它们作为促进睡眠药物的用途。

  公开号：

  US09242970B2
• 作为产物：
  描述：

  (2-(二氟甲氧基)吡啶-4-基)甲醇 、 四溴化碳 、 三苯基膦 在 氮气 、 二氯甲烷 作用下， 以 二氯甲烷 为溶剂， 反应 1.0h， 以afforded 4-(bromomethyl)-2-(difluoromethoxy)pyridine as a yellow oil which的产率得到4-(Bromomethyl)-2-(difluoromethoxy)pyridine
  参考文献：
  名称：

  Lactam derivatives useful as orexin receptor antagonists

  摘要：

  本发明涉及公式(I)的内酰胺衍生物，其中Y，R1，R2和R3如描述中所述，它们的制备，其药学上可接受的盐以及它们作为药物的用途，含有一个或多个公式（I）化合物的药物组合物，特别是它们作为促进睡眠药物的用途。

  公开号：

  US09242970B2

文献信息

• [EN] LACTAM DERIVATIVES USEFUL AS OREXIN RECEPTOR ANTAGONISTS<br/>[FR] DÉRIVÉS DE LACTAME UTILES EN TANT QU'ANTAGONISTES DU RÉCEPTEUR DE L'OREXINE
  申请人：ACTELION PHARMACEUTICALS LTD

  公开号：WO2012063207A1

  公开（公告）日：2012-05-18

  The present invention relates to lactam derivatives of formula (I) wherein Y, R1, R2 and R3 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.

  本发明涉及公式（I）的内酰胺衍生物，其中Y、R1、R2和R3如描述中所述，以及它们的制备方法，其药学上可接受的盐，以及它们作为药物的用途，包括含有一个或多个公式（I）化合物的药物组合物，特别是它们作为促进睡眠的药物受体拮抗剂的用途。
• [EN] PYRANYL ARYL METHYL BENZOQUINAZOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS<br/>[FR] MODULATEURS ALLOSTÉRIQUES POSITIFS DE RÉCEPTEUR M1 DE TYPE PYRANYL-ARYL-MÉTHYL-BENZOQUINAZOLINONE
  申请人：MERCK SHARP & DOHME

  公开号：WO2011025851A1

  公开（公告）日：2011-03-03

  The present invention is directed to pyranyl aryl methyl benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

  本发明涉及式（I）的吡喃基芳基甲基苯并喹唑啉酮化合物，这些化合物是M1受体阳性变构调节剂，可用于治疗M1受体参与的疾病，如阿尔茨海默病、精神分裂症、疼痛或睡眠障碍。该发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在治疗由M1受体介导的疾病中的用途。
• PYRANYL ARYL METHYL BENZOQUINAZOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
  申请人：Kuduk Scott D.

  公开号：US20120157438A1

  公开（公告）日：2012-06-21

  The present invention is directed to pyranyl aryl methyl benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

  本发明涉及式(I)的吡喃基苯基甲基苯并喹唑酮化合物，它们是M1受体正向变构调节剂，可用于治疗M1受体参与的疾病，如阿尔茨海默病、精神分裂症、疼痛或睡眠障碍。该发明还涉及包括该化合物的制药组合物，以及使用该化合物和组合物治疗M1受体介导的疾病。
• LACTAM DERIVATIVES USEFUL AS OREXIN RECEPTOR ANTAGONISTS
  申请人：Aissaoui Hamed

  公开号：US20130237525A1

  公开（公告）日：2013-09-12

  The present invention relates to lactam derivatives of formula (I) wherein Y, R 1 , R 2 and R 3 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.

  本发明涉及式(I)的内酰胺衍生物，其中Y、R1、R2和R3如描述中所述，以及它们的制备方法、药学上可接受的盐和它们作为药物的用途，含有一个或多个式(I)化合物的药物组合物，特别是它们作为促进睡眠的药物。
• Pyranyl Aryl Methyl Benzoquinolinone M1 Receptor Positive Allosteric Modulators
  申请人：Merck Sharp & Dohme Corp.

  公开号：US20140364395A1

  公开（公告）日：2014-12-11

  The present invention is directed to pyranyl aryl methyl benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

  本发明涉及公式（I）的吡喃基苯甲基苯并喹唑酮化合物，其为M1受体正向变构调节剂，可用于治疗M1受体参与的疾病，如阿尔茨海默病、精神分裂症、疼痛或睡眠障碍。本发明还涉及包含该化合物的药物组合物，以及使用该化合物和组合物治疗M1受体介导的疾病的方法。