2-fluoro-3-iodophenol | 897957-00-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 酚类
• 英文名称: 2-fluoro-3-iodophenol
• CAS: 897957-00-5
• 化学式: C₆H₄FIO
• 分子量: 238.0
• InChiKey: SREOHDAFLRMPKV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  20.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-fluoro-3-iodophenol 、 氯甲基甲基醚 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 3.0h， 以3.98 g的产率得到2-fluoro-3-iodomethoxymethoxybenzene
  参考文献：
  名称：

  结合的定向远程金属化-过渡金属催化的交叉偶联策略：Gilvocarcins V，M和E和Arnottin I的糖苷配基的总合成

  摘要：

  关键的定向远程金属化（DreM）-氨基甲酰基迁移策略被用于有效合成天然存在的6H-萘并[1,2 - b ]苯并吡喃-6-一品烟脱氧叶绿素V（1a，方案11）。所需的联芳基氨基甲酸酯33d可以通过高产率的31a铃木偶联反应与受保护的三聚氧化萘偶联伴侣32d进行高产率的合成来制备，该偶联伴侣是通过使用juglone衍生物进行选择性酰化而合成的。在合成的后期阶段，三氟甲磺酸酯39担当了公共中间来安装所需的C-8乙烯基1A（Stille偶联）以及用于制备脱氢福尔霉素类药物M（1b）和E（1c）所需的取代基。对各种保护基团的策略进行了研究，并提供了有关DreM-氨基甲酰基迁移过程中首选哪个基团的见解。从这种全合成过程中学到的战略经验被应用在结构相似的天然产物芦丁素I（2）的成功全合成过程中。

  DOI：

  10.1021/jo9001454
• 作为产物：
  描述：

  o-fluorophenoxytrimethylsilane 在 四甲基乙二胺 、 仲丁基锂 、 碘 、 氯化铵 作用下， 以 四氢呋喃 、 正己烷 、 环己烷 、 水 为溶剂， 反应 8.08h， 以0.200 g的产率得到2-fluoro-3-iodophenol
  参考文献：
  名称：

  结合的定向远程金属化-过渡金属催化的交叉偶联策略：Gilvocarcins V，M和E和Arnottin I的糖苷配基的总合成

  摘要：

  关键的定向远程金属化（DreM）-氨基甲酰基迁移策略被用于有效合成天然存在的6H-萘并[1,2 - b ]苯并吡喃-6-一品烟脱氧叶绿素V（1a，方案11）。所需的联芳基氨基甲酸酯33d可以通过高产率的31a铃木偶联反应与受保护的三聚氧化萘偶联伴侣32d进行高产率的合成来制备，该偶联伴侣是通过使用juglone衍生物进行选择性酰化而合成的。在合成的后期阶段，三氟甲磺酸酯39担当了公共中间来安装所需的C-8乙烯基1A（Stille偶联）以及用于制备脱氢福尔霉素类药物M（1b）和E（1c）所需的取代基。对各种保护基团的策略进行了研究，并提供了有关DreM-氨基甲酰基迁移过程中首选哪个基团的见解。从这种全合成过程中学到的战略经验被应用在结构相似的天然产物芦丁素I（2）的成功全合成过程中。

  DOI：

  10.1021/jo9001454

文献信息

• Organic compounds
  申请人：Novartis AG

  公开号：EP2177518A1

  公开（公告）日：2010-04-21

  3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4-substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula I, wherein the symbols have the meanings defined in the specification.

  3,4-取代的哌啶化合物，这些化合物用于温血动物的诊断和治疗，特别是用于治疗依赖于肾素活性的疾病（=失调）；该类化合物用于制备治疗依赖于肾素活性的疾病的药物制剂；公开了该类化合物在治疗依赖肾素活性的疾病中的用途；包含3,4-取代的哌啶化合物的药物制剂，和/或包括施用3,4-取代的哌啶化合物的治疗方法，3,4-取代的哌啶化合物的制造方法，以及新型中间体及其合成的部分步骤。3,4-二取代哌啶化合物具有式 I、 其中符号具有本说明书中定义的含义。
• TETRAHYDROPYRROLE COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND USE THEREOF
  申请人：Mediconns (Shanghai) Biopharmaceutical Co., Ltd

  公开号：EP3733670A1

  公开（公告）日：2020-11-04

  The present invention discloses a tetrahydropyrrole compound, a preparation method therefor, a pharmaceutical composition containing the same, and a use thereof. The tetrahydropyrrole compound of the present invention is represented by general formula (I). The tetrahydropyrrole compound of the present invention has better inhibitory effects on the positive symptoms of schizophrenia, and the potency thereof is equivalent to or slightly stronger than that of the positive drug olanzapine. In addition, the compound of the present invention has dual inhibitory effects on D2 receptors and DAT receptors, and is effective for treating schizophrenia and improving negative symptoms and cognitive functions, while also reducing vertebral side effects and prolactin secretion.

  本发明公开了一种四氢吡咯化合物、其制备方法、含有该化合物的药物组合物及其用途。本发明的四氢吡咯化合物由通式（I）表示。本发明的四氢吡咯化合物对精神分裂症阳性症状有较好的抑制作用，其药效与阳性药物奥氮平相当或稍强于奥氮平。此外，本发明化合物对D2受体和DAT受体具有双重抑制作用，能有效治疗精神分裂症，改善阴性症状和认知功能，同时还能减少椎体副作用和催乳素分泌。
• SUBSTITUTED PIPERIDINES AS RENIN INHIBITORS
  申请人：Novartis AG

  公开号：EP1833816B1

  公开（公告）日：2009-11-11
• ORGANIC COMPOUNDS
  申请人：Breitenstein Werner

  公开号：US20090312304A1

  公开（公告）日：2009-12-17

  3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4-substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula I,
• Organic Compounds
  申请人：BREITENSTEIN Werner

  公开号：US20110263560A1

  公开（公告）日：2011-10-27

  3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.