3-氨基-4-苯基噻吩-2-羧酸 | 649757-57-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩类
• 中文名称: 3-氨基-4-苯基噻吩-2-羧酸
• 英文名称: 3-amino-4-phenylthiophene-2-carboxylic acid
• CAS: 649757-57-3
• 化学式: C₁₁H₉NO₂S
• 分子量: 219.264
• InChiKey: NTHDUPWFIAOFFY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  91.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  3-氨基-4-苯基噻吩-2-羧酸 生成 3-amino-4-phenylthiophene
  参考文献：
  名称：

  Kirsch, G.; Cagniat, D.; Cagniat, P., Journal of Heterocyclic Chemistry, 1982, vol. 19, p. 443 - 445

  摘要：

  DOI：
• 作为产物：
  描述：

  3-氨基-4-苯基噻吩-2-甲酸甲酯 在 氢氧化钾 作用下， 以 乙醇 为溶剂， 生成 3-氨基-4-苯基噻吩-2-羧酸
  参考文献：
  名称：

  Kirsch, G.; Cagniat, D.; Cagniat, P., Journal of Heterocyclic Chemistry, 1982, vol. 19, p. 443 - 445

  摘要：

  DOI：

文献信息

• [EN] OXETANE SUBSTITUTED THIENO PYRIMIDINONES<br/>[FR] THIÉNOPYRIMIDINONES SUBSTITUÉES PAR OXÉTANE
  申请人：RICHTER GEDEON NYRT

  公开号：WO2012153154A1

  公开（公告）日：2012-11-15

  The present invention provides a compound of Formula (I) or pharmaceutically acceptable salt thereof wherein is selected from the group consisting of unsubstituted aryl and heteroaryl groups and aryl and heteroaryl groups substituted with Q; Q represents fluoro, chloro, bromo, C1-6 straight or branched alkyl, alkylthio, cyano, trihaloalkyl, trihaloalkoxy; Y represents CH or N; R is selected from a group consisting of hydrogen, C1-6 straight or branched alkyl, C1-6 alkoxy, trihaloalkyl, trihaloalkoxy, amino, alkylamino, dialkylamino, hydroxy cyano, acetyl, alkylthio and halo; k is independently an integer 2 or 3; n is an integer from 0 to 2 and m is an integer from 1 to 4 provided that sum of the integers m and n is equal to an integer from 2 to 4. The invention also relates to pharmaceutical compositions containing them, to processes for their preparation, new intermediate compounds thereof and to their use in the treatment and/or prophylaxis of a melanin concentrating hormone receptor 1 and optionally H3 receptor related disease or condition.

  本发明提供了一种式（I）的化合物或其药学上可接受的盐，其中所述的选择自未取代芳基和杂环芳基群以及取代有Q的芳基和杂环芳基群的群组；Q代表氟、氯、溴、C1-6直链或支链烷基、烷基硫、氰基、三卤代烷基、三卤代烷氧基；Y代表CH或N；R选自氢、C1-6直链或支链烷基、C1-6烷氧基、三卤代烷基、三卤代烷氧基、氨基、烷基氨基、二烷基氨基、羟基氰基、乙酰基、烷基硫和卤素的群组；k独立地是整数2或3；n是0到2的整数，m是1到4的整数，前提是整数m和n的总和等于2到4的整数。该发明还涉及含有它们的药物组合物，用于它们的制备方法，其新的中间化合物以及在治疗和/或预防黑色素浓集激素受体1和可选的H3受体相关疾病或症状中的使用。
• Active manganese dioxide promoted cyclization of ortho-(1H-pyrrol-1-yl)aryl and heteroaryl carboxylic acids to 5H-pyrrolo[1,2-a][3,1]benzoxazin-5-one derivatives
  作者：Fedora Grande、Antonella Brizzi、Antonio Garofalo、Francesca Aiello

  DOI：10.1016/j.tet.2013.09.072

  日期：2013.11

  1]benzoxazin-5-one and six of its substituted derivatives have been prepared by active manganese dioxide promoted oxidative cyclization of the corresponding 2-(1H-pyrrol-1-yl)benzoic acids, under mild conditions, in moderate yields. The method was successfully extended to the cyclization of some ortho-(1H-pyrrol-1-yl)heteroaryl carboxylic acids and 2-(1H-indol-1-yl)benzoic acids.

  迄今未知内酯5 ħ -吡咯并[1,2-一个] [3,1]苯并恶嗪-5-酮和其取代的衍生物的6已经制备由活性二氧化锰促进了相应的2-（1-氧化合环ħ -在温和条件下以中等收率得到吡咯-1-基）苯甲酸。该方法已成功地扩展到某些邻-（1 H-吡咯-1-基）杂芳基羧酸和2-（1 H-吲哚-1-基）苯甲酸的环化反应。
• [EN] INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B<br/>[FR] INHIBITEURS DE LA PROTEINE TYROSINE PHOSPHATASE 1B
  申请人：WYETH CORP

  公开号：WO2005081954A2

  公开（公告）日：2005-09-09

  Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted thiophene compounds such as, for example, 2-carboxyl, 3-carboxymethoxy, 5-aryl substituted thiophenes, can inhibit PTPIB and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes.
• Kirsch, G.; Cagniat, D.; Cagniat, P., Journal of Heterocyclic Chemistry, 1982, vol. 19, p. 443 - 445
  作者：Kirsch, G.、Cagniat, D.、Cagniat, P.

  DOI：——

  日期：——