diethyl 2-aminobut-2-enedioate | 3527-16-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: diethyl 2-aminobut-2-enedioate
• 英文别名: Diethyl 2-aminobut-2-enedioate
• CAS: 3527-16-0
• 化学式: C₈H₁₃NO₄
• 分子量: 187.196
• InChiKey: FFZBMYDDXULOPW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  13
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  78.6
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  diethyl 2-aminobut-2-enedioate 、 罗丹明B 在 三乙胺 作用下， 以 1,2-二氯乙烷 为溶剂， 反应 5.5h， 以40%的产率得到
  参考文献：
  名称：

  A highly sensitive fluorescent acidic pH probe based on rhodamine B diethyl-2-aminobutenedioate conjugate and its application in living cells

  摘要：

  A highly sensitive fluorescent acidic pH probe based on rhodamine B-2-aminobutenedioate conjugate, was designed and synthesized. When the H+ concentration falls within the pH range of 4.0-6.5, the spirolactam unit of rhodamine B-2-aminobutenedioate was opened, which resulted in the dramatic enhancement of both fluorescence and absorbance intensity as well as the color change of the solution. Background metal ions showed small or no interference with the detection of H+. Confocal laser scanning microscopy experiments showed that rhodamine B-2-aminobutenedioate can be applied to detect acidic pH variations in living cells with a turn-on signal. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.dyepig.2012.07.012

文献信息

• HIV INTEGRASE INHIBITORS
  申请人：ViiV Healthcare Company

  公开号：US20150225399A1

  公开（公告）日：2015-08-13

  The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.

  本发明具有作为HIV整合酶抑制剂的化合物，因此在抑制HIV复制、预防及/或治疗HIV感染以及治疗艾滋病及/或艾滋病相关综合症方面具有用途。
• Process for preparing pyridine-2,3-dicarboxylic acid compounds
  申请人：Sugai Chemical Ind. Co., Ltd.

  公开号：US04973695A1

  公开（公告）日：1990-11-27

  A process for preparing pyridine-2,3-dicarboxylic acid compounds of the following formula: ##STR1## wherein R.sup.1 and R.sup.3 are, identical or different, each a hydrogen atom or a lower alkyl group, R.sup.2 is a hydrogen atom, a lower alkyl group, or a phenyl-(lower)alkyl group which may have halogen atom or lower alkyl group on its phenyl ring, and R.sup.4 and R.sup.5 are, identical or different, each a lower alkoxy group. The compounds are useful as an intermediate for preparing agricultural chemicals and pharmaceuticals.

  一种制备以下式子的吡啶-2,3-二羧酸类化合物的方法：##STR1## 其中R.sup.1和R.sup.3是相同或不同的氢原子或较低的烷基，R.sup.2是氢原子、较低的烷基或苯基-(较低)烷基，其苯环上可能有卤原子或较低的烷基，而R.sup.4和R.sup.5是相同或不同的较低烷氧基。这些化合物可用作制备农药和制药中间体。
• Hiv Integrase Inhibitors
  申请人：Johns Alvin Brian

  公开号：US20070124152A1

  公开（公告）日：2007-05-31

  The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.

  本发明涉及一种HIV整合酶抑制剂化合物，因此在抑制HIV复制，预防和/或治疗HIV感染以及治疗艾滋病和/或ARC方面具有用途。
• A process for preparation of enantiomerically pure polysubstituted 1,4-dihydropyridines
  申请人：BOEHRINGER MANNHEIM ITALIA S.P.A.

  公开号：EP0383320A1

  公开（公告）日：1990-08-22

  A process for the optical resolution of racemic 1,4-dihydropyridines, containing isothioureido groups. Salification of racemic isothioureas with optically active acids produces diasteroisomeric mixtures of isothiouronium salts, that, using conventional techniques, are separated in the individual components to give optically pure isothioureides of 1,4-dihydropyri­dines and salts thereof with conventional acids. Said optically pure 1,4-dihydropyridines can then be subjected to desulphuration and to different transformations to give other enantiomerically pure and therapeutically useful 1,4-dihydropyridines.

  一种对含有异硫脲基的外消旋 1,4-二氢吡啶进行光学分解的工艺。用光学活性酸盐化外消旋异硫脲，可产生异硫脲鎓盐的二异构体混合物，用常规技术分离各组分，可得到光学纯度为 1,4-二氢吡啶的异硫脲及其与常规酸的盐。上述光学纯度的 1,4-二氢吡啶可以进行脱硫和不同的转化，从而得到其他对映体纯度和治疗用途的 1,4-二氢吡啶。
• Process for preparing pyridine carboxylic acid derivatives
  申请人：HOECHST CELANESE CORPORATION

  公开号：EP0415767A2

  公开（公告）日：1991-03-06

  A method for preparing pyridine carboxylic acid esters by reacting N-hydroxyamino derivatives of the formula: wherein R₅ and R₆ are each independently H, COZ, or CN, provided that they are not both H; or R₅ and R₆ together are -CO-NR₁₀-CO; Z is OR₈ or NR₈R₉; R₈ and R₉are each independently H or alkyl or aryl; or R₈ and R₉ together with the nitrogen atom form an aliphatic or aromatic heterocyclic structures and R₁₀ is hydrogen, alkyl, aryl, hydroxy or an alkoxy of 1-6 carbon atoms; with an α,β-unsaturated aldehyde or ketone is disclosed. In an additional embodiment, an alkene of formula R₅-CH=CH-R₆, wherein R₅ and R₆ are defined as above, is reacted with hydroxylamine or a salt thereof to form N-hydroxylamino derivatives which are then treated as above.

  一种通过与式中的 N-羟基氨基衍生物反应制备吡啶甲酸酯的方法： 其中R₅和R₆各自独立地为H、COZ或CN，但它们不能都是H；或R₅和R₆一起为-CO-NR₁₀-CO；Z为OR₈或NR₈；R₈和R₉各自独立地为H或烷基或芳基；或 R₈ 和 R𠢙 与氮原子一起形成脂肪族或芳香族杂环结构，且 R₁₀ 是氢、烷基、芳基、羟基或 1-6 个碳原子的烷氧基；公开了具有 α、β-不饱和醛或酮的化合物。在另一个实施方案中，式 R₅-CH=CH-R₆（其中 R₅ 和 R₆ 定义如上）的烯烃与羟胺或其盐反应生成 N-羟基氨基衍生物，然后按上述方法处理。