2-fluoro-4-iodo-3-methoxypyridine | 1227580-53-1

• 物质功能分类: 医药中间体
• 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: 2-fluoro-4-iodo-3-methoxypyridine
• CAS: 1227580-53-1
• 化学式: C₆H₅FINO
• 分子量: 253.015
• InChiKey: IVXNIUMDPHLSBV-UHFFFAOYSA-N

物化性质

• 沸点：
  281.1±40.0 °C(Predicted)
• 密度：
  1.903±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  22.1
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-fluoro-4-iodo-3-methoxypyridine 在 四(三苯基膦)钯 、 甲烷磺酸(2-二环己基膦基-2',4',6'-三-异丙基-1,1'-联苯基)(2'-氨基-1,1'-联苯-2-基)钯(II) 、 sodium carbonate 作用下， 以 四氢呋喃 、 1,4-二氧六环 为溶剂， 反应 48.5h， 生成 tert-butyl (2S,4S)-1-[2-(difluoromethyl)-[1]benzofuro[3,2-d]pyrimidin-4-yl]-4-[5-[3-methoxy-2-(methylamino)pyridin-4-yl]-3-[(9S)-9-methyl-2,5-dioxa-8-azaspiro[3.5]nonan-8-yl]pyridin-2-yl]oxypyrrolidine-2-carboxylate
  参考文献：
  名称：

  [EN] PYRIDINE DERIVATIVES WITH N-LINKED CYCLIC SUBSTITUENTS AS CGAS INHIBITORS
  [FR] DÉRIVÉS DE PYRIDINE AYANT DES SUBSTITUANTS CYCLIQUES À LIAISON N EN TANT QU'INHIBITEURS DE CGAS

  摘要：

  The invention relates to new proline derivatives of formula (I) as cGAS inhibitors, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11and G are defined as in claim 1, and prodrugs or pharmaceutically acceptable salts of these compounds for the treatment of diseases such as systemic lupus erythematosus, systemic sclerosis (SSc), non-alcoholic steatotic hepatitis (NASH), interstitial lung disease (ILD) and idiopathic pulmonary fibrosis (IPF).

  公开号：

  WO2022238327A1
• 作为产物：
  描述：

  2-氟-3-甲氧基吡啶 在 正丁基锂 、 碘 作用下， 以 四氢呋喃 、 正己烷 为溶剂， 反应 3.33h， 生成 2-fluoro-4-iodo-3-methoxypyridine
  参考文献：
  名称：

  [EN] 2-PYRIDYLOXY-3-SUBSTITUTED-4-NITRILE OREXIN RECEPTOR ANTAGONISTS
  [FR] ANTAGONISTES DU RÉCEPTEUR DE LA 2-PYRIDYLOXY-3-SUBSTITUÉE-4-NITRILE ORÉXINE

  摘要：

  本发明涉及2-吡啶氧基-3-取代-4-腈化合物，其是促进睡眠荷尔蒙受体的拮抗剂。本发明还涉及使用本文所述的2-吡啶氧基-3-取代-4-腈化合物在治疗或预防神经系统和精神疾病中的用途，其中涉及促进睡眠荷尔蒙受体。本发明还涉及包含这些化合物的制药组合物。本发明还涉及使用这些制药组合物在预防或治疗涉及促进睡眠荷尔蒙受体的疾病中的用途。

  公开号：

  WO2014066196A1

文献信息

• [EN] HYDROXYMETHYL PIPERIDINE OREXIN RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES DES RÉCEPTEURS DES OREXINES DE TYPE PIPÉRIDINE HYDROXYMÉTHYLIQUE
  申请人：MERCK SHARP & DOHME

  公开号：WO2016089722A1

  公开（公告）日：2016-06-09

  The present invention is directed to hydroxymethyl piperidine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.

  本发明涉及羟甲基哌啶类化合物，其为促进睡眠的受体拮抗剂。本发明还涉及所述化合物在潜在的治疗或预防神经系统和精神疾病中的用途，这些疾病涉及促进睡眠的受体。本发明还涉及含有这些化合物的组合物。本发明还涉及利用这些组合物在潜在的预防或治疗涉及促进睡眠的受体的疾病中的用途。
• [EN] HALO AND TRIFLUOROMETHYL SUBSTITUTED OREXIN RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES DES RÉCEPTEURS DE L'OREXINE SUBSTITUÉS PAR DES GROUPES HALO ET TRIFLUOROMÉTHYLE
  申请人：MERCK SHARP & DOHME

  公开号：WO2014176146A1

  公开（公告）日：2014-10-30

  The present invention is directed to halo and trifluoromethyl substituted compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

  本发明涉及卤代和三氟甲基取代化合物，其为促进醒觉素受体拮抗剂。本发明还涉及上述化合物在潜在的神经和精神障碍和疾病的治疗或预防中的应用，其中醒觉素受体参与其中。本发明还涉及包含这些化合物的制药组合物。本发明还涉及这些制药组合物在预防或治疗醒觉素受体参与的这些疾病中的应用。
• AZAINDAZOLE COMPOUNDS
  申请人：Velaparthi Upender

  公开号：US20130184254A1

  公开（公告）日：2013-07-18

  Disclosed are azaindazole compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein W is CR 4 or N; and R 1 , R 2 , R 3 , and R 4 are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.

  本发明涉及式(I)的吡唑嗪化合物，或其药学上可接受的盐，其中W为CR4或N；R1、R2、R3和R4在此定义。本发明还涉及使用这种化合物治疗至少一种CYP17相关疾病的方法，例如癌症，以及包含这种化合物的制药组合物。
• SUBSTITUTED AZAINDAZOLE COMPOUNDS
  申请人：Austin Joel F.

  公开号：US20130231354A1

  公开（公告）日：2013-09-05

  Disclosed are azaindazole compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein: Q is: (i) 5-membered heteroaryl comprising at least one nitrogen heteroatom and substituted with zero to 2 Rg; or (ii) 9- to 10-membered bicyclic heteroaryl selected from Formula (II) and; wherein Ring A is a 5- to 6-membered aryl or heteroaryl fused ring substituted with zero to 2 Rg; and R1, R2, R3, and Rg are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.

  本发明涉及以下式（I）的吡唑吡嗪化合物或其药学上可接受的盐，其中：Q为：（i）包含至少一个氮杂原子的5-成员杂芳基，取代基为零到2个Rg；或（ii）选自式（II）的9-至10-成员双环杂芳基；其中环A为5-至6-成员芳基或杂芳基融合环，取代基为零到2个Rg；R1、R2、R3和Rg如本文所定义。本发明还涉及使用这种化合物治疗至少一种CYP17相关疾病的方法，例如癌症，以及包含这种化合物的制药组合物。
• 2-PYRIDYLOXY-3-SUBSTITUTED-4-NITRILE OREXIN RECEPTOR ANTAGONISTS
  申请人：KUDUK Scott D.

  公开号：US20150291558A1

  公开（公告）日：2015-10-15

  The present invention is directed to 2-pyridyloxy-3-substituted-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-3-substituted-4-nitrile compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

  本发明涉及2-吡啶氧基-3-取代-4-腈化合物，其为促进睡眠激素受体的拮抗剂。本发明还涉及使用本文所述的2-吡啶氧基-3-取代-4-腈化合物在治疗或预防神经和精神障碍和疾病中的应用，其中促进睡眠激素受体参与其中。本发明还涉及包含这些化合物的药物组合物。本发明还涉及使用这些药物组合物在预防或治疗促进睡眠激素受体参与的疾病中的应用。