3-[(2-乙酰氧基)乙基氨基羰基]吡啶 | 83440-03-3

• 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
• 中文名称: 3-[(2-乙酰氧基)乙基氨基羰基]吡啶
• 中文别名: 尼可地尔杂质8
• 英文名称: SG 209
• 英文别名: N-[2-(acetoxy)ethyl]-3-pyridinecarboxamide；3-[(2-acetoxy)ethylaminocarbonyl]pyridine；2-(pyridine-3-carbonylamino)ethyl acetate
• CAS: 83440-03-3
• 化学式: C₁₀H₁₂N₂O₃
• mdl: MFCD00181603
• 分子量: 208.217
• InChiKey: JQICNNKLTFYSLS-UHFFFAOYSA-N

物化性质

• 溶解度：
  DMSO：~24 mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  15
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  68.3
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• 安全说明：
  S22,S24/25
• 海关编码：
  2933399090

反应信息

• 作为反应物：
  描述：

  3-[(2-乙酰氧基)乙基氨基羰基]吡啶 、 碘甲烷 以 硝基甲烷 为溶剂， 生成
  参考文献：
  名称：

  WO2007/38772

  摘要：

  公开号：
• 作为产物：
  描述：

  N-(2-羟乙基)烟酰胺 、 乙酰氯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 3-[(2-乙酰氧基)乙基氨基羰基]吡啶
  参考文献：
  名称：

  WO2007/38772

  摘要：

  公开号：

文献信息

• [EN] PROCESS FOR THE MANUFACTURE OF NICORANDIL<br/>[FR] PROCÉDÉ DE FABRICATION DE NICORANDIL
  申请人：PROCOS SPA

  公开号：WO2012089769A1

  公开（公告）日：2012-07-05

  Disclosed is a process for the synthesis of Nicorandil (1), 2-(nicotinamide)ethyl nitrate, starting from N-(2-hydroxyethyl)nicotinamide (15), using nitration with nitric acid in the presence of acetic anhydride Said synthesis method is particularly advantageous because it solves the safety problems involved in the use of nitric acid as nitrating agent, and allows a product with excellent yields and quality to be isolated.

  揭示了一种合成尼可地尔（1），2-（烟酰胺）乙基硝酸酯的方法，起始物为N-（2-羟乙基）烟酰胺（15），使用乙酸酐存在下的硝化反应。该合成方法特别优越，因为它解决了使用硝酸作为硝化剂所涉及的安全问题，并且允许分离出产量和质量优异的产品。
• 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 Drugs for Dementia
  申请人：Ternansky Robert

  公开号：US20080227806A1

  公开（公告）日：2008-09-18

  The invention is directed to compounds that are prodrugs containing a chemical delivery system (CDS) moiety and a cysteine protease inhibitor moiety. The CDS moiety targets the prodrug to the brain or central nervous system. The cysteine protease inhibitor inhibits cysteine proteases upon release from the prodrug. Cysteine protease inhibitors are effective for treating dementia, Alzheimer's disease and vascular dementia. Targeting the brain or central nervous system offers significant advantages in treating these conditions and diseases. A preferred CDS prodrug is a dihydrotrigoneline CDS moiety coupled to an epoxysuccinyl peptide cysteine protease inhibitor moiety.

  本发明涉及一种含有化学递送系统（CDS）基团和半胱氨酸蛋白酶抑制剂基团的前药化合物。CDS基团将前药定位于大脑或中枢神经系统。半胱氨酸蛋白酶抑制剂在从前药中释放后抑制半胱氨酸蛋白酶。半胱氨酸蛋白酶抑制剂对治疗痴呆症、阿尔茨海默病和血管性痴呆症有效。定位于大脑或中枢神经系统在治疗这些疾病和症状方面具有显著的优势。首选的CDS前药是将二氢三角线CDS基团与环氧丙酰肽半胱氨酸蛋白酶抑制剂基团耦合。
• Capture compounds, collections thereof and methods for analyzing the proteome and complex compositions
  申请人：Kõster Hubert

  公开号：US20100248264A1

  公开（公告）日：2010-09-30

  Capture compounds and collections thereof and methods using the compounds for the analysis of biomolecules are provided. In particular, collections, compounds and methods are provided for analyzing complex protein mixtures, such as the proteome. The compounds are multifunctional reagents that provide for the separation and isolation of complex protein mixtures. Automated systems for performing the methods also are provided.

  提供了捕获化合物及其集合以及使用这些化合物进行生物分子分析的方法。特别地，提供了用于分析复杂蛋白质混合物（如蛋白质组）的集合、化合物和方法。这些化合物是多功能试剂，可用于分离和分离复杂的蛋白质混合物。还提供了执行这些方法的自动化系统。
• 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。