N-(1-methoxyethyl)-3-pyridylcarboxamide | 1060642-55-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: N-(1-methoxyethyl)-3-pyridylcarboxamide
• 英文别名: N-(1-methoxyethyl)-nicotinamide；N-(1-methoxyethyl)pyridine-3-carboxamide
• CAS: 1060642-55-8
• 化学式: C₉H₁₂N₂O₂
• 分子量: 180.206
• InChiKey: GIOASRSJIHWGIV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  51.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  乙烯基三甲氧基硅烷 、 烟酰胺 在 copper diacetate 、 四丁基氟化铵 作用下， 以 二氯甲烷 为溶剂， 反应 2.0h， 以60%的产率得到尼可地尔杂质P
  参考文献：
  名称：

  Direct N-vinylation of aryl and hetaryl carboxamides with trimethoxyvinylsilane

  摘要：

  A general method for direct N-vinlylation of aryl and hetaryl carboxamides with trimethoxyvinylsilane using a copper(II) acetate-TBAF system as catalyst is elaborated. The yield of N-vinyl amides depends strongly on the initial amide and nature of the solvent. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2008.06.117

文献信息

• Novel compounds for the management of aging-related and diabetic vascular complications, process for their preparation, therapeutic and cosmetic uses thereof
  申请人：TORRENT PHARMACEUTICALS LTD.

  公开号：US20030045554A1

  公开（公告）日：2003-03-06

  The invention discloses a new clause of a five membered heterocylic ring compounds of general formula 1 1 and its pharmaceutically or cosmetically acceptable salts, wherein R1, R2, R3, R4, R5, A, B, X and Y are as defined in the specification. The invention also discloses a process for preparation of these compound and their therapeutic and cosmetic applications particularly in the management of aging related and diabetic vascular complications. The compounds in question act by triple action of an AGE (Advanced Glycation Endproducts) breaker, AGE inhibitor and free radical scavenger which make them most suitable in different therapeutic and cosmetic applications. The invention also discloses pharmaceuticals and cosmetic compositions comprising these compounds and method of treatment of diseases caused by accumulation of AGE and/or free radicals in the body cells.

  本发明公开了一种新的通式11的五元杂环化合物及其药学或美容学可接受的盐，其中R1、R2、R3、R4、R5、A、B、X和Y在说明书中定义。本发明还公开了制备这些化合物及其治疗和美容应用的方法，特别是在管理与衰老相关和糖尿病血管并发症方面。所述化合物通过AGE（高级糖基化终产物）断裂剂、AGE抑制剂和自由基清除剂的三重作用发挥作用，使它们在不同的治疗和美容应用中最为适用。本发明还公开了包含这些化合物的药物和化妆品组合物以及治疗由体细胞中AGE和/或自由基积累引起的疾病的方法。
• Novel compounds for the management of aging-related and diabetic vascular complications, process for their preparation and therapeutic uses thereof
  申请人：——

  公开号：US20010018524A1

  公开（公告）日：2001-08-30

  Novel compounds of the pyridinium series useful for the management of diabetes and aging-related vascular complications, including kidney disease, nerve damage, atherosclerosis, retinopathy, dermatological disorders and discoloration of teeth, by breaking preformed AGE, of the general formula I, or pharmaceutically acceptable salts thereof, 1 wherein, R 1 , R 2 , R 3 , X and m are as defined in the specification. Also disclosed is a method for preparation of the compounds of general formula (I) and pharmaceutical composition containing one or more compounds as defined above as active ingredients. Also disclosed is a method of treatment of a diabetic patient by administering the compounds as defined above, either singly or in combination with drugs for antidiabetic therapy.

  本发明涉及一系列新的吡啶系列化合物，可用于管理糖尿病和与衰老相关的血管并发症，包括肾脏疾病、神经损伤、动脉硬化、视网膜病变、皮肤疾病和牙齿变色，通过破坏预先形成的AGE，其通式为I，或其药学上可接受的盐，其中，R1、R2、R3、X和m如规范中所定义。本发明还公开了一种制备通式（I）化合物的方法和含有一种或多种上述化合物作为活性成分的制药组合物。本发明还公开了一种通过单独或与抗糖尿病治疗药物联合使用上述化合物治疗糖尿病患者的方法。
• Composition and method for use of pyridinium derivatives in cosmetic and therapeutic applications
  申请人：Torrent Pharmaceuticals Ltd

  公开号：EP1304101A1

  公开（公告）日：2003-04-23

  The invention discloses a new class of compounds particularly pyridinium derivatives, which have been found to exhibit triple function of a free radical scavenger (antioxidant), AGE breaker and AGE inhibitor, and cosmetic composition comprising these compounds contained in a cosmetically acceptable carrier. The invention also discloses a method of cosmetic application by applying such composition. The invention further discloses a pharmaceutical composition, comprising said compounds useful in scavenging free radicals from the body cells of a mammal, a method of scavenging free radicals from the body cells of a mammal and a method of treating of diseases caused by accumulation of free radicals in the body cells of a mammal by administering a composition made with the compounds of the invention. The invention in addition, also discloses composition and method for inhibiting AGE in a mammal by use of the compounds of the same group.

  本发明公开了一类新化合物，特别是吡啶鎓衍生物，它们被发现具有自由基清除剂（抗氧化剂）、AGE 破坏剂和 AGE 抑制剂的三重功能，还公开了包含在化妆品可接受载体中的这些化合物的化妆品组合物。本发明还公开了一种通过施用此类组合物进行美容的方法。本发明进一步公开了一种药物组合物，其中包含有助于清除哺乳动物体细胞中自由基的所述化合物；一种清除哺乳动物体细胞中自由基的方法；以及一种通过施用用本发明化合物制成的组合物治疗哺乳动物体细胞中自由基积累引起的疾病的方法。此外，本发明还公开了通过使用同组化合物抑制哺乳动物体内 AGE 的组合物和方法。
• Pyridinium compounds useful for the treatment of AGE-related diseases
  申请人：Torrent Pharmaceuticals Ltd

  公开号：EP1243581B1

  公开（公告）日：2005-07-13
• Vinylation of pyridylcarboxamides with vinyltrimethoxysilane
  作者：P. Arsenyan、A. Petrenko、S. Belyakov

  DOI：10.1007/s10593-012-0943-0

  日期：2012.3

  A convenient method has been developed for the direct N-vinylation of pyridylcarboxamides with vinyltrimethoxysilane in the presence of copper(II) acetate and tetrabutylammonium fluoride. The yield of N-vinylamides depends on the nature of the starting amide and the solvent. The molecular structure of the products was confirmed by X-ray structural analysis.