2-(thien-2'-ylmethoxy)phthalimide | 39685-80-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: 2-(thien-2'-ylmethoxy)phthalimide
• 英文别名: N-(thiophen-2-ylmethoxy)phthalimide；N-(thien-2-ylmethoxy)phthalimide；2-(thiophen-2-ylmethoxy)isoindole-1,3-dione
• CAS: 39685-80-8
• 化学式: C₁₃H₉NO₃S
• 分子量: 259.285
• InChiKey: SIVLKUKUNCKWMF-UHFFFAOYSA-N

物化性质

• 沸点：
  415.3±47.0 °C(Predicted)
• 密度：
  1.46±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  74.8
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-(thien-2'-ylmethoxy)phthalimide 在 碳酸氢钠 、 一水合肼 作用下， 以 乙醇 、 乙酸乙酯 、 N,N-二甲基甲酰胺 为溶剂， 反应 4.0h， 生成 1-(Thiophen-2-ylmethoxy)-4,5-dihydro-1H-imidazole-2-thiol
  参考文献：
  名称：

  1-Benzyloxy-4,5-dihydro-1H-imidazol-2-yl-amines, a novel class of NR1/2B subtype selective NMDA receptor antagonists

  摘要：

  Screening of the Roche compound depository led to the identification of (1-benzyloxy-4,5-dihydro-1H-imidazol-2-yl)-butyl amine 4, a structurally novel NR1/2B Subtype selective NMDA receptor antagonist. The structure-activity relationships developed in this series resulted in the discovery of a novel class of potent and selective NMDA receptor blockers displaying activity in vivo. (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(03)00713-3
• 作为产物：
  描述：

  2-噻吩甲醛 在 lithium aluminium tetrahydride 、 三苯基膦 、 偶氮二甲酸二乙酯 作用下， 以 四氢呋喃 为溶剂， 反应 18.5h， 生成 2-(thien-2'-ylmethoxy)phthalimide
  参考文献：
  名称：

  Identification of Human Alanine–Glyoxylate Aminotransferase Ligands as Pharmacological Chaperones for Variants Associated with Primary Hyperoxaluria Type 1

  摘要：

  DOI：

  10.1021/acs.jmedchem.2c00142

文献信息

• Control of parasites in animals by the use of novel trifluoromethanesulfonanilide oxime ether derivatives
  申请人：Meyer Gerhard Adam

  公开号：US20060063841A1

  公开（公告）日：2006-03-23

  Novel trifluoromethanesulfonanilide oxime ether compounds useful for controlling endo and/or ectoparasites in the environment are provided, together with methods of making the same, and methods of using the inventive compounds to treat parasite infestations in vivo or ex vivo.

  提供了一种新型三氟甲磺酰苯胺肟醚化合物，可用于控制环境中的内寄生虫和/或外寄生虫，同时提供了制备这些化合物的方法，以及利用这些创新化合物治疗体内或体外寄生虫感染的方法。
• Synthesis of 1,2-oxazaheterocycles containing an isoindolone moiety from<i>N</i>-Hydroxyphthalimide
  作者：Alexander Bartovic、Bernard Decroix、P. Netchitaïlo

  DOI：10.1002/jhet.5570370426

  日期：2000.7

  and halogenomethylaryl derivatives. The resulting aryloxy phthalimides 4a-c were reduced to hydroxylactams 5a-c which cyclized in acidic conditions. A Wittig reaction on 5a using carbethoxymethylidenetriphenylphosphorane gave the corresponding acid 6 which treated in Friedel and Crafts conditions led to the isoxazolinone 8 by cleavage of the benzyl CO bond.

  由N-羟基邻苯二甲酰亚胺3和卤代甲基芳基衍生物开发了异吲哚并苯并恶嗪酮1a和噻嗪并异吲哚并酮1b，c的合成物。将所得的芳氧基邻苯二甲酰亚胺4a-c还原为羟基内酰胺5a-c，其在酸性条件下环化。使用碳乙氧基甲基亚甲基三苯基苯基膦在5a上进行维蒂希反应，得到相应的酸6，该酸在Friedel和Crafts条件下处理，通过裂解苄基C O键产生异恶唑啉酮8。
• Penicillins having a 6.beta.-(.alpha.-etherified oximino) acylamido group
  申请人：Glaxo Laboratories Limited

  公开号：US03932385A1

  公开（公告）日：1976-01-13

  The invention provides novel antibiotic compounds which are 6.beta.-acylamidopenam-3-carboxylic acids, and non-toxic derivatives thereof, characterized in that the acylamido group has the structure ##EQU1## WHERE R is a hydrogen atom or an organic group and R.sup.a is an etherifying monovalent organic group linked to the oxygen atom through a carbon atom. The compounds may be either syn or anti isomers or may exist as mixtures e.g. containing at least 75 percent of one isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive organisms including penicillinase - producing staphylococci coupled with high activity against strains of the gram-negative organism Haemophilus influenzae. The invention is also concerned with the administration of the compounds.

  本发明提供了新型抗生素化合物，即6-β-酰胺基青霉烷-3-羧酸及其非毒性衍生物，其特征在于酰胺基具有结构式##EQU1##其中R为氢原子或有机基团，R.sup.a为通过碳原子连接到氧原子的醚化一价有机基团。这些化合物可以是syn或anti异构体，也可以存在混合物中，例如含有至少75％的一个异构体。这些抗生素化合物对一系列革兰氏阳性菌具有高抗菌活性，包括产青霉素酶的葡萄球菌，并对革兰氏阴性菌流感嗜血杆菌菌株具有高活性。本发明还涉及该化合物的给药。
• Cephalosporins having (.alpha.-etherified oximino)acylamido groups at
  申请人：Glaxo Laboratories Limited

  公开号：US03971778A1

  公开（公告）日：1976-07-27

  The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof characterized in that the acylamido group has the structure ##EQU1## where R is a hydrogen atom or an organic group and R.sup.a is an etherifying monovalent organic group linked to the oxygen atom through a carbon atom. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range or gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.

  该发明提供了一种新型抗生素化合物，即7-β-酰胺基头孢-3-乙烯-4-羧酸及其非毒性衍生物，其特征在于酰胺基具有以下结构：##EQU1## 其中R是氢原子或有机基团，R.sup.a是通过碳原子与氧原子连接的醚化一价有机基团。这些化合物是同构体或存在至少75％的同构体混合物。这些抗生素化合物具有高抗菌活性，可对一系列革兰氏阳性和革兰氏阴性微生物产生高度的稳定性，其尤其对各种革兰氏阴性微生物产生的β-内酰胺酶具有高度的稳定性。该发明还涉及该化合物的给药。
• Pencillins having a 6.beta.-(.alpha.-etherified oximino) acylamido group
  申请人：Glaxo Laboratories Limited

  公开号：US03975376A1

  公开（公告）日：1976-08-17

  The invention provides novel antibiotic compounds which are 6.beta.-acylamidopenam-3-carboxylic acids, and nontoxic derivatives thereof, characterized in that the acylamido group has the structure ##EQU1## WHERE R is a hydrogen atom or an organic group and R.sup.a is an etherifying monovalent organic group linked to the oxygen atom through a carbon atom. The compounds may be either syn or anti isomers or may exist as mixtures e.g. containing at least 75% of one isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive organisms including penicillinase - producing staphylococci coupled with high activity against strains of the gram-negative organism Haemophilus influenzae. The invention is also concerned with the administration of the compounds.

  本发明提供了新型抗生素化合物，它们是6-β-酰胺基青霉烯-3-羧酸及其非毒性衍生物，其特征在于酰胺基具有以下结构：##EQU1## 其中R是氢原子或有机基团，R.sup.a是通过碳原子与氧原子连接的醚化一价有机基团。这些化合物可以是syn或anti异构体，也可以存在于混合物中，例如至少含有75％的一个异构体。这些抗生素化合物对包括产青霉素酶的葡萄球菌在内的一系列革兰氏阳性菌株具有高抗菌活性，并且对流感嗜血杆菌的菌株也具有高活性。本发明还涉及这些化合物的给药。