N-2-methoxyethyl 2-phenylacetamide | 124932-14-5

• 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-2-methoxyethyl 2-phenylacetamide
• 英文别名: phenyl-acetic acid-(2-methoxy-ethylamide)；Phenyl-essigsaeure-(2-methoxy-aethylamid)；N-(2-Methoxyethyl)-2-phenylacetamide
• CAS: 124932-14-5
• 化学式: C₁₁H₁₅NO₂
• mdl: MFCD00784008
• 分子量: 193.246
• InChiKey: GAIMHZBLTGWUPF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  14
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.363
• 拓扑面积：
  38.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  苯乙酰氯 、 alkaline earth salt of/the/ methylsulfuric acid 生成 N-2-methoxyethyl 2-phenylacetamide
  参考文献：
  名称：

  Behrens et al., Journal of Biological Chemistry, 1948, vol. 175, p. 771,778

  摘要：

  DOI：

文献信息

• Direct conversion of esters to secondary amides using tin(II) reagents
  作者：Wei-Bo Wang、José A. Restituyo、Eric J. Roskamp

  DOI：10.1016/s0040-4039(00)79291-4

  日期：1993.11

  We have developed two new procedures for the direct conversion of esters to secondary amides. In our first procedure, secondary amides can be prepared in 83–98% yield starting from glycol esters. Addition of Sn[N(TMS)2]2 and a primary amine to the glycol ester generates an intermediate tin(II) alkoxy amide, which delivers the amino group intramolecularly to give the amide. A second general procedure

  我们已经开发了两种新方法，可将酯直接转化为仲酰胺。在我们的第一个步骤中，可以从乙二醇酯开始以83-98％的产率制备仲酰胺。向二醇酯中添加Sn [N（TMS）2 ] 2和伯胺可生成中间体锡（II）烷氧基酰胺，该中间体可分子内递送氨基，从而生成酰胺。制备仲酰胺的第二种通用​​方法是从甲酯开始。用衍生自Sn [N（TMS）2 ] 2，Me 2 NCH 2 CH 2 OH和伯酰胺的锡试剂处理甲酯，收率87-98％。
• [EN] NOVEL SULFAMIDE PIPERAZINE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS AND PHARMACEUTICAL USE THEREOF<br/>[FR] NOUVEAUX DÉRIVÉS DE SULFAMIDE PIPÉRAZINE À TITRE D'INHIBITEURS DE PROTÉINES TYROSINE KINASES ET LEUR UTILISATION PHARMACEUTIQUE
  申请人：LEO PHARMA AS

  公开号：WO2012093169A1

  公开（公告）日：2012-07-12

  The invention relates to compounds of general Formula (I), Wherein R1, R2, R3, R4, R5, m, n are defined herein, and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates thereof, for use - alone or in combination with one or more other pharmaceutically active compounds- in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disesase, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation.

  该发明涉及一般式(I)的化合物，其中R1、R2、R3、R4、R5、m、n在此处定义，并且其药用可接受的盐、前药、水合物或溶剂化合物，用于单独或与一个或多个其他药用活性化合物结合在一起，在治疗中使用，作为JAK激酶和蛋白酪氨酸激酶抑制剂，用于预防、治疗或改善疾病及其并发症，包括例如牛皮癣、特应性皮炎、酒渣鼻、狼疮、多发性硬化症、类风湿关节炎、I型糖尿病、哮喘、癌症、自身免疫性甲状腺疾病、溃疡性结肠炎、克罗恩病、阿尔茨海默病、白血病、眼部疾病如糖尿病视网膜病变和黄斑变性以及其他自身免疫性疾病和免疫抑制希望的适应症，例如在器官移植中。
• A convenient synthesis of amides from carboxylic acids and primary amines
  作者：J. Cossy、C. Pale-Grosdemange

  DOI：10.1016/s0040-4039(00)99121-4

  日期：1989.1

  A convenient method for the formation of carboxamides from carboxylic acids and primary amines in the presence of molecular sieves is described. This process is very chemoselective.

  描述了一种在分子筛存在下由羧酸和伯胺形成羧酰胺的简便方法。这个过程是非常化学选择性的。
• Mesoporous structured silica – An improved catalyst for direct amide synthesis and its application to continuous flow processing
  作者：James W. Comerford、Thomas J. Farmer、Duncan J. Macquarrie、Simon W. Breeden、James H. Clark

  DOI：10.3998/ark.5550190.0013.719

  日期：——

  heterogeneous amidation catalyst based on thermal treatment of amorphous K60 silica, however the loading of catalyst required was high for some reactions. We report her ein our further development of a series of heterogeneous catalysts based on structured silica (SBA) that retain all the green credentials of the previously described amorphous silica, but with increased efficiency. These catalysts were then utilised

  我们最近发表了基于无定形 K60 二氧化硅热处理的有效、可重复使用和良性多相酰胺化催化剂的详细信息，但是对于某些反应，所需的催化剂负载量很高。我们报告她进一步开发了一系列基于结构化二氧化硅 (SBA) 的多相催化剂，这些催化剂保留了先前描述的无定形二氧化硅的所有绿色证书，但效率更高。然后将这些催化剂用于连续流动系统，在显着缩短反应时间的情况下实现了出色的转化率。
• SUBSTITUTED CYCLOPENTYL-AZINES AS CASR-ACTIVE COMPOUNDS
  申请人：Schou Soren Christian

  公开号：US20130345194A1

  公开（公告）日：2013-12-26

  The invention relates to compounds of general Formula (I), Wherein R 1 , R 2 , R 3 , R 4 , R 5 , m, n are defined herein, and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disesase, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation.

  本发明涉及一般式（I）的化合物，其中R1、R2、R3、R4、R5、m、n在此定义，并且其药物可接受的盐、前药、水合物或溶剂化物，用于治疗，单独或与一个或多个其他药物活性化合物结合使用，作为JAK激酶和蛋白酪氨酸激酶抑制剂，用于预防、治疗或改善疾病及其并发症，包括例如牛皮癣、特应性皮炎、酒渣鼻、狼疮、多发性硬化症、类风湿性关节炎、1型糖尿病、哮喘、癌症、自身免疫性甲状腺疾病、溃疡性结肠炎、克罗恩病、阿尔茨海默病、白血病、眼病例如糖尿病视网膜病变和黄斑变性以及其他自身免疫性疾病和需要免疫抑制的适应症，例如器官移植。