4-Acetylamino-phenol-carbamat | 90557-93-0

• 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: 4-Acetylamino-phenol-carbamat
• 英文别名: 1-acetylamino-4-carbamoyloxy-benzene；1-Acetylamino-4-carbamoyloxy-benzol；Carbamidsaeure-(4-acetamino-phenylester)；(4-Acetamidophenyl) carbamate
• CAS: 90557-93-0
• 化学式: C₉H₁₀N₂O₃
• 分子量: 194.19
• InChiKey: NLZLISRHGNJKJT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  81.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-溴-2-乙基丁酰溴 、 4-Acetylamino-phenol-carbamat 在 2,3-二甲基苯胺 作用下， 生成 (2-ethyl-2-bromo-butyryl)-carbamic acid-(4-acetylamino-phenyl ester)
  参考文献：
  名称：

  DE318803

  摘要：

  公开号：
• 作为产物：
  描述：

  (4-硝基苯基)氨基甲酸酯 在 盐酸 、 sodium acetate 、 钯 、 溶剂黄146 作用下， 生成 4-Acetylamino-phenol-carbamat
  参考文献：
  名称：

  DE318803

  摘要：

  公开号：

文献信息

• A MEDICAMENT FOR TREATING INFLUENZA CHARACTERIZED BY COMBINING A CAP-DEPENDENT ENDONUCLEASE INHIBITOR AND AN ANTI-INFLUENZA DRUG
  申请人：Shionogi & Co., Ltd.

  公开号：US20200261481A1

  公开（公告）日：2020-08-20

  A medicament characterized in that (A) a compound represented by the formula (I): its pharmaceutically acceptable salt, or a solvate thereof, wherein P is hydrogen or a group to form a prodrug; A 1 is CR 1A R 1B , S or O; A 2 is CR 2A R 2B , S or O; A 3 is CR 3A R 3B , S or O; A 4 is each independently CR 4A R 4B , S or O; the number of hetero atoms among atoms constituting the ring which consists of A 1 , A 2 , A 3 , A 4 , nitrogen atom adjacent to A 1 and carbon atom adjacent to A 4 is 1 or 2; R 1A and R 1B are each independently hydrogen, halogen, alkyl or the like; R 2A and R 2B are each independently hydrogen, halogen, alkyl, or the like; R 3A and R 3B are each independently hydrogen, halogen, alkyl, or the like; R 4A are each independently hydrogen, halogen, alkyl, or the like; R 4B are each independently hydrogen, halogen, alkyl, or the like; R 3A and R 3B may be taken together with an adjacent carbon atom to form non-aromatic carbocycle or non-aromatic heterocycle; n is any integer of 1 to 2; and R 1 is or the like, is combined with (B) compound(s) having an anti-influenza activity, its pharmaceutically acceptable salt or a solvate thereof and/or an antibody having anti-influenza activity, is useful for treating or preventing influenza.

  一种药物，其特征在于（A）由以下式（I）表示的化合物： 其药学上可接受的盐，或其溶剂合物， 其中 P为氢或形成前药的基团; A 1 为CR 1A R 1B 、S或O; A 2 为CR 2A R 2B 、S或O; A 3 为CR 3A R 3B 、S或O; A 4 分别为独立的CR 4A R 4B 、S或O; 构成由A 1 、A 2 、A 3 、A 4 、邻接到A 1 的氮原子和邻接到A 4 的碳原子的环的原子中的杂原子数为1或2; R 1A 和R 1B 分别为独立的氢、卤素、烷基或类似物; R 2A 和R 2B 分别为独立的氢、卤素、烷基或类似物; R 3A 和R 3B 分别为独立的氢、卤素、烷基或类似物; R 4A 分别为独立的氢、卤素、烷基或类似物; R 4B 分别为独立的氢、卤素、烷基或类似物; R 3A 和R 3B 可以与相邻的碳原子结合形成非芳香碳环或非芳香杂环; n为1到2的任意整数; 和 R 1 为 或类似物， 与具有抗流感活性的（B）化合物，其药学上可接受的盐或其溶剂合物和/或具有抗流感活性的抗体结合，用于治疗或预防流感。
• [EN] ONE POT ACYLATION OF AROMATIC AMINES<br/>[FR] ACYLATION MONOTOPE D'AMINES AROMATIQUES
  申请人：COUNCIL SCIENT IND RES

  公开号：WO2013008256A1

  公开（公告）日：2013-01-17

  The present invention provides a cost effective, environmental friendly and efficient, one pot decarboxylative acylation of aromatic/heteroaromatic primary /secondary amine using diethyl malonate (DEM) to obtain corresponding homologated amides in good yield with a high degree of purity.

  本发明提供了一种经济、环保且高效的方法，使用乙酸二乙酯（DEM）对芳香/杂环原/次要胺进行一锅脱羧酰化反应，以获得相应的同系物酰胺，产率高且纯度高。
• ACETAMINOPHEN CONJUGATES, COMPOSITIONS AND METHODS OF USE THEREOF
  申请人：Acorda Therapeutics, Inc.

  公开号：US20140243407A1

  公开（公告）日：2014-08-28

  Acetaminophen conjugates are provided, which have an acetaminophen moiety covalently linked to a second moiety. The conjugates provided may have one or more advantageous properties, including increased water solubility as compared to acetaminophen, reduced toxicity profile as compared to acetaminophen and an altered pharmacokinetic profile. Formulations comprising the conjugates are also provided, as are methods of using the conjugates and kits comprising the conjugates.

  提供了乙酰氨基酚结合物，其中乙酰氨基酚基团与第二基团共价连接。提供的结合物可能具有一个或多个优点，包括与乙酰氨基酚相比具有增加的水溶性，与乙酰氨基酚相比具有降低的毒性剖面和改变的药代动力学剖面。还提供了包含结合物的配方，以及使用结合物的方法和包含结合物的工具包。
• Medicament for treating influenza characterized by combining a Cap-dependent endonuclease inhibitor and an anti-influenza drug
  申请人：Shionogi & Co., Ltd.

  公开号：US11040048B2

  公开（公告）日：2021-06-22

  A medicament characterized in that (A) a compound represented by the formula (I): its pharmaceutically acceptable salt, or a solvate thereof, wherein P is hydrogen or a group to form a prodrug; A1 is CR1AR1B, S or O; A2 is CR2AR2B, S or O; A3 is CR3AR3B, S or O; A4 is each independently CR4AR4B, S or O; the number of hetero atoms among atoms constituting the ring which consists of A1, A2, A3, A4, nitrogen atom adjacent to A1 and carbon atom adjacent to A4 is 1 or 2; R1A and R1B are each independently hydrogen, halogen, alkyl or the like; R2A and R2B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B are each independently hydrogen, halogen, alkyl, or the like; R4A are each independently hydrogen, halogen, alkyl, or the like; R4B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B may be taken together with an adjacent carbon atom to form non-aromatic carbocycle or non-aromatic heterocycle; n is any integer of 1 to 2; and R1 is or the like, is combined with (B) compound(s) having an anti-influenza activity, its pharmaceutically acceptable salt or a solvate thereof and/or an antibody having anti-influenza activity, is useful for treating or preventing influenza.

  一种药物，其特征在于 (A) 由式 (I) 所代表的化合物： 其药学上可接受的盐或其溶液、 其中 P 是氢或可形成原药的基团； A1 是 CR1AR1B、S 或 O A2 是 CR2AR2B，S 或 O A3 是 CR3AR3B，S 或 O； A4各自独立地为CR4AR4B、S或O； 在由 A1、A2、A3、A4、与 A1 相邻的氮原子和与 A4 相邻的碳原子构成的环的原子中，杂原子的数目为 1 或 2； R1A 和 R1B 各自独立地为氢、卤素、烷基或类似物； R2A 和 R2B 各自独立地为氢、卤素、烷基或类似物； R3A 和 R3B 各自独立地为氢、卤素、烷基或类似物； R4A 各自独立地为氢、卤素、烷基或类似物； R4B 各自独立地为氢、卤素、烷基或类似物； R3A 和 R3B 可与相邻碳原子一起形成非芳香族碳环或非芳香族杂环； n 是 1 到 2 的任意整数；以及 R1 是 或类似内容、 与（B）具有抗流感活性的化合物、其药学上可接受的盐或其溶解物和/或具有抗流感活性的抗体结合，可用于治疗或预防流感。
• An Improved Synthesis of Carbamates
  作者：Bernard Loev、Minerva F. Kormendy

  DOI：10.1021/jo01047a033

  日期：1963.12