2-ethoxy-1-ethoxycarbonyl-1,2,3,4-tetrahydroquinoline | 24030-89-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 2-ethoxy-1-ethoxycarbonyl-1,2,3,4-tetrahydroquinoline
• 英文别名: EEDQ；1-Ethoxycarbonyl-2-ethoxy-1,2,3,4-tetrahydro-chinolin；2-Ethoxy-1-carbethoxy-1,2,3,4-terahydrochinolin；N-ethoxy-carbonyl-2-ethoxy-1,3-dihydroquinoline；1-ethoxycarbonyl-2-ethoxy-3,4-dihydroquinoline；N-ethoxycarbonyl-2-ethoxy-1,3-dihydroquinoline；ethyl 2-ethoxy-3,4-dihydro-2H-quinoline-1-carboxylate
• CAS: 24030-89-5
• 化学式: C₁₄H₁₉NO₃
• 分子量: 249.31
• InChiKey: QDSCNNCJPLTQLA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  38.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-乙氧基-1-乙氧碳酰基-1,2-二氢喹啉 在 platinum(IV) oxide 氢气 作用下， 以 乙醇 为溶剂， 反应 12.0h， 生成 2-ethoxy-1-ethoxycarbonyl-1,2,3,4-tetrahydroquinoline
  参考文献：
  名称：

  Cremin, Denis J.; Hegarty, Anthony F.; Begley, Michael J., Journal of the Chemical Society. Perkin transactions II, 1980, p. 412 - 420

  摘要：

  DOI：
• 作为试剂：
  描述：

  (3alpha,5beta,7alpha)-3-[(乙氧羰基)氧基]-7-羟基胆烷-24-酸甲酯 在 甲醇 、 sodium tetrahydroborate 、 potassium chromate 、 四氧化锇 、 2-ethoxy-1-ethoxycarbonyl-1,2,3,4-tetrahydroquinoline 、 氢溴酸 、 溴 、 溶剂黄146 、 三乙胺 、 potassium hydroxide 、 锌 作用下， 生成 glycoβ-muricholic acid
  参考文献：
  名称：

  [EN] INHIBITORS OF THE FARNESOID X RECEPTOR AND USES IN MEDICINE
  [FR] INHIBITEURS DU RÉCEPTEUR FARNÉSOÏDE X ET LEURS UTILISATIONS EN MÉDECINE

  摘要：

  公开号：

  WO2015017813A3

文献信息

• Preparing pyrazolopyrimidinone derivatives for the treatment of impotence
  申请人：——

  公开号：US20030176696A1

  公开（公告）日：2003-09-18

  The present invention relates to the method for preparing pyrazolopyrimidinone derivatives and their pharmaceutically acceptable salts having efficacy on the treatment of impotence, one of male sexual dysfunctions. The method according to the present invention comprises the steps of chlorosufonation the pyrazolamide, followed by amination with amine and intramolecular cyclization. The method provides the pyrazolopyrimidinone derivatives and their pharmaceutically acceptable salts with high yield and in an economic manner.

  本发明涉及一种制备吡唑吡咯啉酮衍生物及其药学上可接受的盐的方法，该衍生物可用于治疗男性性功能障碍之一的阳痿。根据本发明的方法包括对吡唑酰胺进行氯磺化，然后用胺进行氨基化和分子内环化。该方法以高产率和经济的方式提供了吡唑吡咯啉酮衍生物及其药学上可接受的盐。
• [EN] A PROCESS FOR PREPARING PYRAZOLOPYRIMIDINONE DERIVATIVES FOR THE TREATMENT OF IMPOTENCE<br/>[FR] PROCEDE DE PREPARATION DE DERIVES DE PYRAZOLOPYRIMIDINONE UTILES POUR TRAITER L'IMPUISSANCE
  申请人：DONG A PHARM CO LTD

  公开号：WO2001098304A1

  公开（公告）日：2001-12-27

  The present invention relates to the method for preparing pyrazolopyrimidinone derivatives and their pharmaceutically acceptable salts having efficacy on the treatment of impotence, one of male sexual dysfunctions. The method according to the present invention comprises the steps of chlorosufonation the pyrazolamide, followed by amination with amine and intramolecular cyclization. The method provides the pyrazolopyrimidinone derivatives and their pharmaceutically acceptable salts with high yield and in an economic manner.

  本发明涉及一种制备吡唑并嘧啶酮衍生物及其药学上可接受的盐的方法，该方法对治疗男性性功能障碍之一的阳痿具有疗效。根据本发明的方法，包括对吡唑酰胺进行氯磺化，然后与胺进行氨化和分子内环化。该方法以高收率和经济方式提供了吡唑并嘧啶酮衍生物及其药学上可接受的盐。
• [EN] PYRAZOLOPYRIMIDINONE DERIVATIVES FOR THE TREATMENT OF IMPOTENCE<br/>[FR] DERIVES DE PYRAZOLOPYRIMIDINONE UTILES POUR TRAITER L'IMPUISSANCE
  申请人：DONG A PHARM CO LTD

  公开号：WO2000027848A1

  公开（公告）日：2000-05-18

  The present invention relates to pyrazolopyrimidinone derivatives of formula (1), their preparation method and pharmaceutical compositions containing the said derivatives. The compounds have efficacy on the treatment of impotence, one of male sexual dysfunctions with the side effects reduced.

  本发明涉及式（1）的吡唑嘧啶酮衍生物，其制备方法和包含所述衍生物的制药组合物。该化合物具有治疗阳痿的功效，是男性性功能障碍之一，其副作用也得到了减轻。
• 2-Aza-substituted 1-carbadethiapen-2-EM-3-carboxylic acids
  申请人：Merck & Co., Inc.

  公开号：EP0208889A1

  公开（公告）日：1987-01-21

  Disclosed are 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids 1, where the generic 2-aza group includes azido, acylamino, amino, alkylamino, dialkylamino, triazolyl, triazolinyl, aziridinyl, and their pharmaceutically acceptable salt, ester, anhydride and amide derivatives which are useful as antibiotics. Also disclosed are processes for the preparation of I from the known, appropriately substituted bicyclic keto ester II via the 2-azido central intermediate III: wherein R" is H or CH,, preferably beta-methyl; R6, and R7 are independently hydrogen, linear, branched or cyclic C1-C5alkyl, which can be substituted with fluoro, hydroxy, protected hydroxy, sulfoxy, amino, protected amino, wherein R' and R' taken together can also be C2-C4 alkylidene, similarly substituted; with the proviso that both R6 and R7 are not unsubstituted alkyl, R' and R2 are, inter alia, hydrogen, alkyl, acyl, and can be joined to form a ring comprising 3 to 7 atoms; Ra is hydrogen, a salt cation, a removable protecting group, or a pharmaceutically acceptable ester moiety. Also disclosed are pharmaceutical compositions comprising such compounds.

  本发明涉及2-aza取代的1-卡巴德噻吩-2-乙烯-3-羧酸1，其中通用的2-aza基团包括偶氮基、酰胺基、氨基、烷基氨基、二烷基氨基、三唑基、三唑啉基、环氧丙基和它们的药学上可接受的盐、酯、无水物和酰胺衍生物，其作为抗生素有用。还公开了从已知的适当取代的双环酮酯II通过2-偶氮中间体III制备I的过程：其中R"为H或CH，优选为β-甲基；R6和R7独立地为氢、线性、支链或环状C1-C5烷基，可被氟、羟基、保护羟基、磺酰氧基、氨基、保护氨基取代，其中R'和R'在一起也可以是C2-C4烷基亚甲基，同样被取代；条件是R6和R7都不是未取代的烷基，R'和R2是氢、烷基、酰基等，可以连接形成包含3到7个原子的环；Ra是氢、盐阳离子、可移除的保护基或药学上可接受的酯基。还公开了包含这些化合物的制药组合物。
• Use of perfluoroalkyl-containing metal complexes as contrast media in MR-imaging for visualization of plaque, tumors and necroses
  申请人：——

  公开号：US20030072713A1

  公开（公告）日：2003-04-17

  The invention relates to the use of perfluoroalkyl-containing metal complexes that have a critical micelle formation concentration <10 −3 mol/l, a hydrodynamic micelle diameter (2 Rh)>1 nm and a proton relaxivity in plasma (R 1 )>10 l/mmol·s) as contrast media in MR imaging for visualization of plaque, lymph nodes, infarcted and necrotic tissue and for independent visualization of necrotic tissue and tumor tissue.

  本发明涉及使用临界胶束形成浓度小于10-3mol/l，水动力学胶束直径（2Rh）大于1nm，血浆中质子弛豫时间（R1）大于10l/mmol·s的含有全氟烷基的金属配合物作为MR成像的对比介质，用于可视化斑块、淋巴结、梗死和坏死组织以及独立可视化坏死组织和肿瘤组织。