5-methoxycarbonyl-2-thiophenecarboxylic acid hydrazide | 133380-70-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩类
• 英文名称: 5-methoxycarbonyl-2-thiophenecarboxylic acid hydrazide
• 英文别名: 5-hydrazinocarbonyl-thiophene-2-carboxylic acid methyl ester；methyl 5-hydrazinocarbonyl-2-thiophenecarboxylate；methyl 5-(hydrazinecarbonyl)thiophene-2-carboxylate
• CAS: 133380-70-8
• 化学式: C₇H₈N₂O₃S
• 分子量: 200.218
• InChiKey: SIVVJBBURGGGPJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  110
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  5-methoxycarbonyl-2-thiophenecarboxylic acid hydrazide 在 sodium hydroxide 、 氯化亚砜 、 三乙胺 作用下， 以 乙醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 6.0h， 生成 5-(5-phenyl-1,3,4-oxadiazol-2-yl)-2-thiophenecarboxylic acid
  参考文献：
  名称：

  5-杂芳基-2-噻吩羧酸：恶唑和恶二唑

  摘要：

  报道了带有烷基和芳基取代的恶唑和恶二唑环的新型噻吩-2-羧酸的合成。关键前体5-甲酰基-2-噻吩羧酸的顺序官能化提供了中间体羧酸酯，其通过碱性裂解被转化为所需的酸。

  DOI：

  10.1002/jhet.5570280104
• 作为产物：
  描述：

  5-醛基-2-噻吩甲酸 在 氯化亚砜 、 jones reagent 、 sodium carbonate 、 肼 作用下， 以 氯仿 、 N,N-二甲基甲酰胺 、 丙酮 为溶剂， 反应 3.5h， 生成 5-methoxycarbonyl-2-thiophenecarboxylic acid hydrazide
  参考文献：
  名称：

  5-杂芳基-2-噻吩羧酸：恶唑和恶二唑

  摘要：

  报道了带有烷基和芳基取代的恶唑和恶二唑环的新型噻吩-2-羧酸的合成。关键前体5-甲酰基-2-噻吩羧酸的顺序官能化提供了中间体羧酸酯，其通过碱性裂解被转化为所需的酸。

  DOI：

  10.1002/jhet.5570280104

文献信息

• [EN] PYRAZOLONE COMPOUNDS AND THROMBOPOIETIN RECEPTOR ACTIVATOR<br/>[FR] COMPOSES DE PYRAZOLONE ET ACTIVATEUR DU RECEPTEUR DE LA THROMBOPOIETINE
  申请人：NISSAN CHEMICAL IND LTD

  公开号：WO2004033433A1

  公开（公告）日：2004-04-22

  A preventive, therapeutic or improving agent for diseases against which activation of the thrombopoietin receptor is effective or a platelet increasing agent, which contains a thrombopoietin receptor activator represented by the formula (1): wherein A is a C?2-14#191 aryl group, B is a hydrogen atom, a C?1-6#191 alkyl group, a C?1-3#191 alkyl group substituted with one or more fluorine atoms or a C?2-14#191 aryl group, D is a hydrogen atom, a C?1-6#191 alkyl group, a C?1-3#191 alkyl group substituted with one or more fluorine atoms or a C?2-14#191 aryl group, and E is a C?2-14#191 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the activator or a solvate thereof, as an active ingredient.

  一种预防、治疗或改善针对血小板生成素受体激活有效的疾病的药剂或增加血小板的药剂，其中包含由式（1）表示的血小板生成素受体激活剂：其中A是C?2-14#191芳基，B是氢原子，C?1-6#191烷基，一个或多个氟原子取代的C?1-3#191烷基或C?2-14#191芳基，D是氢原子，C?1-6#191烷基，一个或多个氟原子取代的C?1-3#191烷基或C?2-14#191芳基，E是C?2-14#191芳基，激活剂的互变异构体、前药或药用可接受的盐或其溶剂，作为活性成分。
• [EN] 3-ALKYLIDENEHYDRAZINO SUBSTITUTED HETEROARYL COMPOUNDS AS THROMBOPOIETIN RECEPTOR ACTIVATORS<br/>[FR] UTILISATION DE COMPOSES HETEROARYLES A SUBSTITUTION 3-ALKYLIDENEHYDRAZINO EN TANT QU'ACTIVATEURS DU RECEPTEUR DE LA THROMBOPOIETINE
  申请人：NISSAN CHEMICAL IND LTD

  公开号：WO2004108683A1

  公开（公告）日：2004-12-16

  A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14; aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10; alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14; aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.

  化合物的结构式（1）如下：其中A是氮原子或CR4，B是氧原子、硫原子或NR9（但当A是氮原子时，B不是NH），R1是C2-14芳基，L1是键，CR10R11、氧原子、硫原子或NR12，X是OR13、SR13或NR14NR15，R2是氢原子、甲酰基、C1-10烷基或类似物，L2是键或类似物，L3是键，CR17R18、氧原子、硫原子或NR19，L4是键，CR20R21、氧原子、硫原子或NR22，Y是氧原子、硫原子或NR23，R3是C2-14芳基、化合物的互变异构体、前药或药学上可接受的盐或其溶剂化合物。
• 3-substituted-2-oxindole derivatives
  申请人：Pfizer Inc.

  公开号：US05047554A1

  公开（公告）日：1991-09-10

  This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.

  这项发明涉及新型的3-取代-2-噁唑烷酮衍生物，这些衍生物是前列腺素H.sub.2合酶、5-脂氧合酶和白细胞介素-1生物合成的抑制剂。该发明的化合物在慢性炎症性疾病的治疗中可用作前列腺素H.sub.2合酶和白细胞介素-1生物合成的抑制剂，本身也可作为镇痛、抗炎和抗关节炎药物。本发明还涉及包含所述3-取代-2-噁唑烷酮衍生物的药物组合物；抑制前列腺素H.sub.2合酶和白细胞介素-1生物合成的方法；以及使用这些化合物治疗哺乳动物的慢性炎症性疾病。此外，本发明还涉及某些新型羧酸，可用作本发明的3-取代-2-噁唑烷酮衍生物的合成中间体，以及一种制备这些衍生物的方法。
• Thiophene and furan 2,5-dicarboxamides useful in the treatment of cancer
  申请人：BioChem Pharma Inc.

  公开号：US20020137947A1

  公开（公告）日：2002-09-26

  A novel compound which inhibits certain integrins, particularly &agr; v integrins. Additionally, the novel compound may be used in a method of treating tumors or cancer which comprises administering a pharmaceutically effective amount of the compound to a patient. Additionally, the novel compound may be used in a method of inhibiting angiogensis. Finally, a method of producing the novel compound is disclosed.

  一种新的化合物，可以抑制某些整合素，特别是αv整合素。此外，这种新化合物可用于治疗肿瘤或癌症的方法，包括向患者施用化合物的药效有效量。此外，这种新化合物可用于抑制血管生成的方法。最后，还披露了一种生产这种新化合物的方法。
• 2-carboxy-thiophene derivatives
  申请人：Pfizer Inc.

  公开号：US05300655A1

  公开（公告）日：1994-04-05

  This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.

  本发明涉及新型的3-取代-2-氧化吲哚衍生物，其是前列腺素H.sub.2合酶、5-脂氧合酶和白细胞介素-1生物合成的抑制剂。本发明中的化合物本身作为前列腺素H.sub.2合酶和白细胞介素-1生物合成的抑制剂以及作为治疗慢性炎症性疾病的镇痛、抗炎和抗关节炎药物是有用的。本发明还涉及包含所述3-取代-2-氧化吲哚衍生物的制药组合物；抑制前列腺素H.sub.2合酶和白细胞介素-1生物合成的方法；以及使用该化合物治疗哺乳动物的慢性炎症性疾病。此外，本发明还涉及某些新型羧酸，其作为制备本发明的3-取代-2-氧化吲哚衍生物的中间体，以及制备3-取代-2-氧化吲哚衍生物的过程。