N-[(4-磺酰胺)苯基]丙烯酰胺 | 2621-99-0

• 物质功能分类: 化学试剂 - 有机试剂 - 酰胺
• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: N-[(4-磺酰胺)苯基]丙烯酰胺
• 中文别名: N-[4-(磺酰胺)苯基]丙烯酰胺；N-[4-(磺酰胺)苯基]丙烯酰胺ASPAA
• 英文名称: N-[4-(aminosulfonyl)phenyl]acrylamide
• 英文别名: N-acryloyl-sulfanilic acid amide；N-Acryloyl-sulfanilsaeure-amid；N-(4-sulfamoylphenyl)acrylamide；N-<4-(Sulfamoyl)-phenyl>-acrylamid；4-Sulfamoyl-N-acryloyl-anilin；N-(4-(Aminosulphonyl)phenyl)acrylamide；N-(4-sulfamoylphenyl)prop-2-enamide
• CAS: 2621-99-0
• 化学式: C₉H₁₀N₂O₃S
• mdl: MFCD00587450
• 分子量: 226.256
• InChiKey: RINSWHLCRAFXEY-UHFFFAOYSA-N

物化性质

• 熔点：
  215 °C
• 密度：
  1.387±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  97.6
• 氢给体数：
  2
• 氢受体数：
  4

安全信息

• 海关编码：
  2935009090
• 储存条件：
  干燥避光保存。

制备方法与用途

概述

N-[(4-磺酰胺)苯基]丙烯酰胺(ASPAA)单体可以均聚或与其它单体共聚合成具有药理活性的聚合物，制成水溶性、毒副作用小且具有良好缓释作用的大分子药物。由于磺酰胺基具有一定的碱溶性，ASPAA与丙烯酸酯类等单体的共聚物可用于制备可碱显影、显影宽容度和耐印力等性能良好的平版印刷及计算机直接制版版材。

制备

将1.00g磺胺和1.41mL吡啶加入到30mL 1，4-二恶烷中。逐滴加入0.49mL丙烯酰氯，并在室温下搅拌3小时。随后，向溶液中加入1M HCl，使用乙酸乙酯进行萃取。萃取液用盐水和无水硫酸钠干燥后除去溶剂，得到纯度足以用于后续步骤的粗产物。

反应信息

• 作为反应物：
  描述：

  1-(2-吡啶基)哌嗪 、 N-[(4-磺酰胺)苯基]丙烯酰胺 以 二甲基亚砜 为溶剂， 反应 16.0h， 以77%的产率得到3-[4-(2-吡啶基)-1-哌嗪基]-N-(4-氨基磺酰基苯基)丙酰胺
  参考文献：
  名称：

  1-2-(Pyridinyl)piperazine derivatives with antianaphylactic, antibronchospastic and mast cell stabilizing activities

  摘要：

  New 1-(2-pyridinyl)piperazine derivatives were synthesized and tested as inhibitors of the reaginic passive cutaneous anaphylaxis in the rat (PCA), of the histamine-induced bronchospasm in the guinea pig, and of the rat mesenteric mast cell degranulation induced by compound 48/80. On the basis of test results, a series of N-(substituted phenyl)-omega-[4-(2-pyridinyl)-1-piperazinyl]alkanamides was prepared. The nature of substituents at the anilide ring strongly influenced mast cell stabilizing activity, whereas it was less determining in the case of the other two tests. No clear correlation between the most common physicochemical parameters (pi, sigma, Vw volume) of substituents and activity could be detected. With regard to the position of substituents at the anilide ring, the rank order of potency, in the PCA and bronchoconstriction tests, was para greater than meta greater than ortho. Introduction of substituents in the 1-(2-pyridinyl)piperazinyl moiety of the N-(substituted phenyl)propanamide derivatives hardly affected activity, or the effect was deleterious. Some of the new compounds exhibited a simultaneous remarkable activity in all the three assays employed.

  DOI：

  10.1021/jm00384a002
• 作为产物：
  描述：

  磺胺 、 丙烯酰氯 在 三乙胺 作用下， 以 丁酮 为溶剂， 反应 3.0h， 以10.26 g的产率得到N-[(4-磺酰胺)苯基]丙烯酰胺
  参考文献：
  名称：

  Polymeric drug based on sulfanilamide: synthesis, antimicrobial and drug releasing studies

  摘要：

  在三乙胺的存在下，使用磺胺噻唑和丙烯酰氯在0-5°C下合成了N-（（4-氨基磺酰基）苯基）丙烯酰胺（APA）。采用甲乙酮（MEK）作为溶剂，过苯甲酰过氧化物（BPO）作为自由基引发剂，采用溶液聚合技术进行2-羟乙基丙烯酸酯（HEA）和丙烯酸（AA）的同聚和共聚合反应，得到了相应的单体和聚合物。所有单体和聚合物均经过红外光谱和核磁共振技术表征。对这些单体和聚合物进行了抗微生物活性测试，针对五种不同的ATCC菌株微生物（大肠杆菌（25922）、铜绿假单胞菌（27853）、克雷伯菌（70063）、伤寒沙门氏菌（6539）和金黄色葡萄球菌（25923））。讨论了共聚单体中除了活性药物部分外的其他成分对抗菌活性的影响。当与AA和HEA共聚合时，APA对革兰氏阳性菌的抗菌活性得到了增强。将聚合物制成薄膜形式，用于药物释放研究。使用UV分光光度计在268 nm处监测药物释放速率。监测了pH和温度对药物释放速率的影响，并发现释放速率取决于共聚单体、介质的pH和温度。

  DOI：

  10.1211/jpp.59.9.0004

文献信息

• [EN] TRANSGLUTAMINASE TG2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF<br/>[FR] INHIBITEURS DE TRANSGLUTAMINASE TG2, COMPOSITIONS PHARMACEUTIQUES ET LEURS PROCÉDÉS D'UTILISATION
  申请人：CHDI INC

  公开号：WO2011060321A1

  公开（公告）日：2011-05-19

  Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.

  本文提供了某些化合物和药学上可接受的盐。还提供了包括至少一种化合物或其中的药学上可接受的盐以及一种或多种药学上可接受的载体的药物组合物。描述了治疗对转谷氨酰胺酶TG2活性抑制产生响应的患有某些疾病状态的患者的方法。这些疾病状态包括神经退行性疾病，如亨廷顿病。还描述了治疗方法，包括单独给予至少一种化合物或其中的药学上可接受的盐，或者将至少一种化合物或其中的药学上可接受的盐与一种或多种其他治疗剂结合给予。
• Image forming material and ammonium compound
  申请人：FUJI PHOTO FILM CO., LTD.

  公开号：US20030143481A1

  公开（公告）日：2003-07-31

  An image forming material includes an image forming layer containing a water-insoluble and alkali-soluble resin, a light-heat converting agent and a compound represented by the following general formula (1). In general formula (1), R 1 to R 3 independently represent an organic group, where R 1 represents a residue forming a ring containing a N 1 atom, R 2 and R 3 may bond to each other to form a ring or at least one of R 2 and R 3 may bond to R 1 to form a ring and X − represents a conjugate base of an organic acid or inorganic acid. The ring containing the N 1 atom is preferably a piperidine ring. 1

  一种图像形成材料包括一个图像形成层，其中包含一种水不溶性且碱溶性的树脂、一种光热转换剂和一种由下列通式（1）表示的化合物。在通式（1）中，R1到R3独立地表示有机基团，其中R1表示形成一个含有N1原子的环的残基，R2和R3可以结合形成一个环，或者R2和R3中至少一个可以与R1结合形成一个环，X-表示有机酸或无机酸的共轭碱基。含有N1原子的环最好是吡啶环。
• Image-formation material and infrared absorber
  申请人：——

  公开号：US20020015911A1

  公开（公告）日：2002-02-07

  A heat mode-applicable image-formation material having high sensitivity and excellent image-forming property, and a novel infrared absorber which can be suitably used in this material. The present invention relates to a substrate carrying thereon an image-formation layer which contains an infrared absorption agent. The agent has at least one surface orientation group in the molecule, and solubility of the image-formation layer in an alkaline aqueous solution is changed by action of radiation in the near-infrared range. Preferable as the infrared absorbing agent is an infrared absorber comprising, in a molecule thereof, a fluorine-containing substituent which have at least 5 fluorine atoms, or a polymethine chain of at least 5 carbon atoms and an alkyl group of at least 8 carbon atoms, said alkyl group being connected to the polymethine chain via any of nitrogen, oxygen and sulfur.

  一种适用于热模式的高灵敏度和优异成像性能的图像形成材料，以及一种新型红外吸收剂，可适当地用于该材料中。本发明涉及一种携带有图像形成层的基板，该层含有红外吸收剂。该剂分子中至少有一个表面取向基团，并且通过近红外范围的辐射作用，可以改变碱性水溶液中图像形成层的溶解度。作为红外吸收剂，最好选用含有至少5个氟原子的含氟取代基或至少5个碳原子的聚甲烷链和至少8个碳原子的烷基，所述烷基通过氮、氧和硫中的任何一种与聚甲烷链连接。
• POSITIVE RESIST FLUID AND POSITIVE RESIST COMPOSITION
  申请人：——

  公开号：US20020081518A1

  公开（公告）日：2002-06-27

  The present invention provides a positive resist fluid excellent in the storage stability of the fluid and in defocus latitude depended on line pitch, and a positive photoresist composition for far ultraviolet exposure which forms a resist pattern having excellent defocus latitude depended on line pitch and has excellent sensitivity to short-wavelength exposure lights. The positive resist fluid comprises a resin which contains repeating units represented by formula (I) as defined in the specification, a photo-acid generator, and a solvent and the positive photoresist composition for far ultraviolet exposure comprises a resin which contains both alkali-soluble groups protected by groups containing an alicyclic hydrocarbon structure and represented by at least one of formulae (pI) to (pVI) and groups represented by formula (qI): —A—X—R 5 as defined in the specification.

  本发明提供了一种具有优异流体储存稳定性和依赖于线间距离的离焦容限的正性光阻液体，以及用于远紫外线曝光的正性光阻组合物，该组合物形成具有依赖于线间距离的优异离焦容限的阻抗图案，并对短波长曝光光具有优异的敏感性。该正性光阻液体包括根据规范中定义的式(I)表示的重复单元的树脂、光酸发生剂和溶剂，而用于远紫外线曝光的正性光阻组合物包括树脂，该树脂包含由至少一个式(pI)到式(pVI)之一表示的含有脂环烃结构的基团保护的碱溶性基团和由式(qI)表示的基团：—A—X—R5。
• Ink composition for electrostatic ink-jet recording and method of ink-jet recording
  申请人：Kasai Seishi

  公开号：US20050070630A1

  公开（公告）日：2005-03-31

  An ink composition for electrostatic ink-jet recording comprises: a dispersion medium; and a charged particle comprising a colorant, wherein the charged particle contains at least one of an onium salt compound and an onium salt group-containing polymer. A method of ink jet recording comprises an ink droplet of the ink composition by using an electrostatic field.

  一种用于静电喷墨记录的墨水组合物包括：分散介质；以及包含着色剂的带电粒子，其中所述带电粒子包含至少一种onium盐化合物和onium盐基聚合物中的一种。一种喷墨记录的方法包括使用静电场将墨水组合物的墨滴喷出。