N-(3-hydroxyphenyl)methanesulfonamide | 71290-40-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-(3-hydroxyphenyl)methanesulfonamide
• CAS: 71290-40-9
• 化学式: C₇H₉NO₃S
• mdl: MFCD04151187
• 分子量: 187.219
• InChiKey: DJQWZMOQUBMZGR-UHFFFAOYSA-N

物化性质

• 熔点：
  96-96.5 °C
• 沸点：
  354.4±44.0 °C(Predicted)
• 密度：
  1.458±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.142
• 拓扑面积：
  74.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  N-(3-hydroxyphenyl)methanesulfonamide 、 2,4,6-三甲氧基苯甲醛 在 sodium tetrahydroborate 作用下， 以 四氢呋喃 为溶剂， 反应 4.0h， 以89%的产率得到N-(3-hydroxyphenyl)-N-(2,4,6-trimethoxybenzyl)methanesulfonamide
  参考文献：
  名称：

  Hepatoselectivity of statins: Design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors

  摘要：

  4-Sulfamoyl pyrroles were designed as novel hepatoselective HMG-CoA reductase inhibitors (statins) to reduce myalgia, a statin-induced adverse effect. The compounds were prepared via a [3 + 2] cycloaddition of a Munchnone with a sulfonamide-substituted alkyne. We identified compounds with greater selectivity for hepatocytes compared to L6-myocytes than rosuvastatin and atorvastatin. There was an inverse correlation of myocyte potencies and ClogP values. A number of analogs were effective at reducing cholesterol in acute and chronic in vivo models but they lacked sufficient chronic in vivo activity to warrant further development. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.11.124
• 作为产物：
  描述：

  甲基磺酰氯 、 3-氨基苯酚 在 氯化钠 、 乙酸乙酯 、 碳酸氢钠 、 aqueous solution 、 sodium hydroxide 、 盐酸 、 Sodium sulfate-III 作用下， 以 吡啶 为溶剂， 反应 18.0h， 以3.3 g (yield=80%) of N-(3-hydroxyphenyl)methanesulfonamide were obtained as an oil的产率得到N-(3-hydroxyphenyl)methanesulfonamide
  参考文献：
  名称：

  IMIDAZOPYRIDINE DERIVATIVES USEFUL IN TREATING DIABETES

  摘要：

  本发明涉及以下一般式I的咪唑吡啶衍生物，以及它们作为药物的用途，特别是用于治疗和/或预防糖尿病、其并发症和/或相关病理。

  公开号：

  US20150182507A1

文献信息

• ANTI-CANCER PHOSPHONATE ANALOGS
  申请人：Boojamra Constantine G.

  公开号：US20100022467A1

  公开（公告）日：2010-01-28

  The invention is related to phosphorus substituted anti-cancer compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

  本发明涉及磷取代的抗癌化合物、含有这些化合物的组合物以及包括给予这些化合物的治疗方法，还涉及用于制备这些化合物的过程和中间体。
• Imidazopyridine derivatives useful in treating diabetes
  申请人：METABRAIN RESEARCH

  公开号：US09381191B2

  公开（公告）日：2016-07-05

  The present invention relates to imidazopyridine derivatives of the following general formula I: and to their use as a drug, in particular in treating and/or preventing diabetes, its complications and/or associated pathologies.

  本发明涉及以下一般式I的咪唑吡啶衍生物，以及它们作为药物的用途，特别是用于治疗和/或预防糖尿病、其并发症和/或相关病理状态。
• KINASE INHIBITORY PHOSPHONATE ANALOGS
  申请人：Cannizzaro Carina

  公开号：US20090181930A1

  公开（公告）日：2009-07-16

  The invention is related to phosphorus substituted kinase inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

  该发明涉及磷取代的激酶抑制剂化合物，含有这种化合物的组合物，包括给予这种化合物的治疗方法，以及用于制备这种化合物的有用过程和中间体。
• [EN] UROLITHIN DERIVATIVES AND METHODS OF USE THEREOF<br/>[FR] DÉRIVÉS D'UROLITHINE ET LEURS PROCÉDÉS D'UTILISATION
  申请人：VANDRIA SA

  公开号：WO2022162471A1

  公开（公告）日：2022-08-04

  Disclosed are compounds, compositions, and methods useful for treating neuronal and mitochondrial diseases.

  本发明涉及用于治疗神经元和线粒体疾病的化合物、组合物和方法。
• A Mild Synthesis of Aryl Triflates Enabling the Late‐Stage Modification of Drug Analogs and Complex Peptides
  作者：Stefan Schiesser、Joanna Ceklarz、Johanna Kollback、Lucie Borowiec、Julia Fagerlund、Shakiba Vahdat、Marika Lindhagen、Okky Dwichandra Putra

  DOI：10.1002/chem.202301421

  日期：2023.7.26

  triflates using a newly discovered reagent in presence of a fluoride source. The reactions are generally complete within a few minutes at room temperature. The mild conditions allow the late-stage O-triflation of complex peptides bearing challenging side chains like arginine and histidine. We show that aryl triflates can be an interesting moiety for medicinal chemistry.

  我们报告了一种非常方便的策略，使用新发现的试剂在氟化物源存在下将苯酚转化为相应的芳基三氟甲磺酸酯。反应通常在室温下几分钟内完成。温和的条件允许带有挑战性侧链（如精氨酸和组氨酸）的复杂肽进行后期O-三氟甲基化。我们证明芳基三氟甲磺酸酯可能是药物化学中一个有趣的部分。