N-(2,3-二甲氧基苯基)乙酰胺 | 121639-09-6

• 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-(2,3-二甲氧基苯基)乙酰胺
• 中文别名: N-（2,3-二甲氧基苯基）乙酰胺
• 英文名称: N-(2,3-dimethoxyphenyl)acetamide
• 英文别名: 2,3-dimethoxyacetanilide；acetic acid-(2,3-dimethoxy-anilide)；Essigsaeure-(2,3-dimethoxy-anilid)；3-Acetamino-brenzcatechin-dimethylaether；3-Acetamino-veratrol
• CAS: 121639-09-6
• 化学式: C₁₀H₁₃NO₃
• mdl: MFCD05864317
• 分子量: 195.218
• InChiKey: XRMPXEQSASRWAC-UHFFFAOYSA-N

物化性质

• 熔点：
  81-83°C

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  47.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-(2,3-二甲氧基苯基)乙酰胺 生成 2,3-二甲氧基-5,6-二硝基-苯胺
  参考文献：
  名称：

  Vermeulen, Recueil des Travaux Chimiques des Pays-Bas, 1929, vol. 48, p. 970

  摘要：

  DOI：
• 作为产物：
  描述：

  2.3-Dimethoxybenzoylazid 在 三乙胺 作用下， 以 二氯甲烷 、 苯 为溶剂， 反应 21.0h， 生成 N-(2,3-二甲氧基苯基)乙酰胺
  参考文献：
  名称：

  Acetamidoquinone and acetamidohydroxy derivatives as inhibitors for both dihydroxyacetamido epoxidase and dehydrogenase

  摘要：

  A series of monohydroxy and dihydroxyacetanilides, acetamidoquinones and bromoacetamidoquinones have been synthesised and tested as substrates and/or inhibitors of highly purified dihydroxyacetamido epoxidase (DHAE) and dihydroxy acetamido dehydrogenase (DHADH) from Streptomyces LL-C10337. None was found to act as substrates but many selectively inhibit the enzymes. Kinetic analysis has shown that all the compounds act as reversible competitive inhibitors with respect to the substrates 2,5-dihydroxyacetanilide and 2,3-epoxy-1,4-benzoquinone-5-acetanilide. Monohydroxy acetanilides. showed weak inhibition to these enzymes compared to the dihydroxy derivatives while the more powerful inhibitors were the benzoquinoneacetanilide and its 5-bromo equivalent. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0968-0896(01)00403-5

文献信息

• Safety and Tolerability of Bolus Intravenous Colistin in Acute Respiratory Exacerbations in Adults with Cystic Fibrosis
  作者：Steven P Conway、Christine Etherington、James Munday、Martin H Goldman、Joanna J Strong、Mandy Wootton

  DOI：10.1345/aph.19370

  日期：2000.11

  To assess the safety and tolerability of bolus intravenous doses of colistin during acute respiratory exacerbations in adults with cystic fibrosis and chronic Pseudomonas aeruginosainfection.

  Twelve patients with acute exacerbations of cystic fibrosis were enrolled in a Phase I open-label study. On day 1, patients received three doses of colistin 2 mega-units (160 mg), reconstituted in 50 mL of NaCl 0.9%, by infusion over 30 minutes three × daily. On days 2, 3, and 4, the same dose of colistin was administered by bolus injection three × a day over five minutes after reconstitution in 20, 15, and 10 mL of NaCl 0.9%, respectively. The injection was given by a nurse or physician using a hand-held syringe. If the latter dose was tolerated, it was continued for the remaining eight days of the study. If any dose was not tolerated, treatment reverted to the previously tolerated concentration, which was continued throughout the remainder of the study.

  No serious adverse events occurred during the course of the trial. Patients without total indwelling venous access systems experienced mild to moderate injection pain. There were no clinically significant changes in renal function.

  This study indicates that the administration of bolus intravenous colistin as 2 mega-units (160 mg) in 10 mL of NaCl 0.9% three × a day is safe. It is well-tolerated by patients with total indwelling venous access systems.

  评估囊性纤维化成人急性呼吸道恶化期间静脉推注多粘菌素的安全性和耐受性。方法：12名急性囊性纤维化恶化患者参加了一项I期开放标签研究。第1天，患者每天三次通过30分钟输注方式接受3剂多粘菌素2兆单位（160毫克），在0.9%氯化钠50毫升中重新溶解。第2、3和4天，相同剂量的多粘菌素在重新溶解于分别为20、15和10毫升的0.9%氯化钠后，每天三次通过5分钟推注方式给予。注射由护士或医生使用手持注射器进行。如果后一剂量耐受，将继续在研究的其余8天中使用。如果任何剂量不耐受，治疗将恢复到先前耐受的浓度，并在研究的其余部分中继续使用。结果：在试验过程中未发生严重不良事件。没有完全留置静脉通路系统的患者经历了轻度至中度注射疼痛。肾功能没有临床上显著变化。结论：该研究表明，每天三次以10毫升0.9%氯化钠中的2兆单位（160毫克）推注静脉多粘菌素是安全的。对于完全留置静脉通路系统的患者来说，这种方法是耐受良好的。
• Aerobic oxidative homocoupling reaction of anilides using heterogeneous metal catalysts
  作者：Shigenobu Fujimoto、Kenji Matsumoto、Takayuki Iwata、Mitsuru Shindo

  DOI：10.1016/j.tetlet.2017.01.075

  日期：2017.3

  We have developed a heterogeneous catalytic oxidative homocoupling reaction of dimethoxyanilides under an oxygen atmosphere. The resulting homo-dimers are useful for the construction of heterocycles, demonstrating the potential of heterogeneous metal catalysts.

  我们已经开发了在氧气氛下二甲氧基苯胺的非均相催化氧化均偶联反应。所得的均二聚体可用于杂环的构建，证明了多相金属催化剂的潜力。
• Spironolactone in the Treatment of Congestive Heart Failure
  作者：Stanley J Lloyd、Vincent F Mauro

  DOI：10.1345/aph.10104

  日期：2000.11

  To evaluate evidence supporting the use of spironolactone in managing congestive heart failure.

  Literature accessed through MEDLINE (January 1966–December 1999) and cross-referencing of selected articles. Search terms included spironolactone and heart failure.

  Heart failure is a leading cause of morbidity and mortality. Through aldosterone antagonism, spironolactone may be an effective pharmacotherapeutic addition to patients not responding to standard drug therapy for heart failure.

  Clinical trials have demonstrated that, in patients with heart failure, spironolactone improves laboratory indices, quality of life, and morbidity. Recently, spironolactone has been demonstrated to improve the survival of patients with New York Heart Association (NYHA) III or IV heart failure.

  Spironolactone use should be considered in patients with NYHA Class III or IV heart failure.

  目标：评估支持螺内酮在管理充血性心力衰竭中的应用的证据。 数据来源：通过MEDLINE（1966年1月至1999年12月）和所选文章的交叉引用获取的文献。搜索词包括螺内酮和心力衰竭。 数据综合：心力衰竭是发病率和死亡率的主要原因。通过醛固酮拮抗作用，螺内酮可能是对于对心力衰竭标准药物治疗没有反应的患者的有效药物治疗补充。 结果：临床试验表明，在心力衰竭患者中，螺内酮改善了实验室指标、生活质量和发病率。最近，螺内酮已被证明可以改善纽约心脏协会（NYHA）III或IV级心力衰竭患者的生存率。 结论：应考虑在纽约心脏协会III或IV级心力衰竭患者中使用螺内酮。
• [EN] FGFR4 INHIBITORS<br/>[FR] INHIBITEURS DE FGFR4
  申请人：EISAI R&D MAN CO LTD

  公开号：WO2015057963A1

  公开（公告）日：2015-04-23

  Provided herein are compounds of Formula I and Formula II useful as FGFR4 inhibitors, as well as methods of use of the same.

  本文提供的I和II式化合物可用作FGFR4抑制剂，并提供了使用它们的方法。
• Monocyclic benzamides of 3- or 4-substituted 4-(aminomethyl)-piperidine derivatives
  申请人：——

  公开号：US20030078427A1

  公开（公告）日：2003-04-24

  The present invention of compounds of formula (I) 1 a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R 1 is C 1-6 alkyloxy, C 2-6 alkenyloxy or C 2-6 alkynyl-oxy; R 2 is hydrogen, C 1-6 alkyl C 1-6 alkyloxy; R 3 is hydrogen or halo; R 4 is hydrogen or C 1-6 alkyl; R 5 is hydrogen or C 1-6 alkyl; L is C 3-6 cycloalkyl, C 5-6 cycloalkanone, C 2-6 alkenyl, or L is a radical of formula-Alk-R 6 —, Alk-X—R 7 , —Alk-Y—C(═O)—R 9 , or —Alk-Y—C(═O)—NR 11 R 12 wherein each Alk is C 1-12 alkanediyl; and R 6 is hydrogen, cyano, C 1-6 alkylsulfonylamino, C 3-6 cycloalkyl, C 5-6 cyclo-alkanone, or a heterocyclic ringsystem; R 7 is hydrogen, C 1-6 alkyl, hydroxyC 1-6 alkyl, C 3-6 cycloalkyl, or a heterocyclic ringsystem; X is O, S, SO 2 or NR 8 ; said R 8 being hydrogen or C 1-6 alkyl; R 9 is hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkyloxy or hydroxy; Y is NR 10 or a direct bond; said R 10 being hydrogen, or C 1-6 alkyl; R 11 and R 12 each independently are hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, or R 11 and R 12 combined with the nitrogen atom may form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.

  本发明涉及式（I）化合物，其立体化学异构体形式，其N-氧化物形式或其药学上可接受的酸加成盐，其中R1为C1-6烷氧基，C2-6烯氧基或C2-6炔氧基；R2为氢，C1-6烷基或C1-6烷氧基；R3为氢或卤素；R4为氢或C1-6烷基；R5为氢或C1-6烷基；L为C3-6环烷基，C5-6环戊酮，C2-6烯基，或L为式-Alk-R6—，Alk-X—R7，—Alk-Y—C(═O)—R9或—Alk-Y—C(═O)—NR11R12的基团，其中每个Alk为C1-12烷二基；R6为氢，氰基，C1-6烷基磺酰氨基，C3-6环烷基，C5-6环戊酮或杂环环系；R7为氢，C1-6烷基，羟基C1-6烷基，C3-6环烷基或杂环环系；X为O，S，SO2或NR8；其中R8为氢或C1-6烷基；R9为氢，C1-6烷基，C3-6环烷基，C1-6烷氧基或羟基；Y为NR10或直接键；其中R10为氢或C1-6烷基；R11和R12各自独立地为氢，C1-6烷基，C3-6环烷基，或R11和R12与氮原子结合可以形成可选择取代的吡咯烷基，哌啶基，哌嗪基或4-吗啉基环。公开了制备所述产品的过程，包含所述产品的配方以及其作为药物的用途，特别是用于治疗与胃排空障碍有关的疾病。