5-Oxo-8-ethyl-5.8-dihydropyrido(2.3-d)pyrimidin-6-carbonsaeure | 34259-53-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶并嘧啶类
• 英文名称: 5-Oxo-8-ethyl-5.8-dihydropyrido(2.3-d)pyrimidin-6-carbonsaeure
• 英文别名: 6-Carboxy-5,8-dihydro-8-aethyl-5-oxopyrido<2,3-d>pyrimidin；8-ethyl-5-oxo-5,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid；5-Oxo-8-ethyl-5,8-dihydro-pyrido(2,3-d)pyrimidine-6-carboxylic acid；8-ethyl-5-oxopyrido[2,3-d]pyrimidine-6-carboxylic acid
• CAS: 34259-53-5
• 化学式: C₁₀H₉N₃O₃
• 分子量: 219.2
• InChiKey: LXAUTRAHQVROAT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  83.4
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  5-Oxo-6-carbethoxy-8-ethyl-5.8-dihydropyrido(2.3-d)pyrimidin 、 、 disodium;carbonate 在 水 作用下， 以 溶剂黄146 为溶剂， 反应 0.33h， 以of 5-oxo-8-ethyl-5,8-dihydro-pyrido-(2,3-d)pyrimidine-6-carboxylic acid is obtained的产率得到5-Oxo-8-ethyl-5.8-dihydropyrido(2.3-d)pyrimidin-6-carbonsaeure
  参考文献：
  名称：

  Process for the preparation of an

  摘要：

  有价值的抗菌8-烷基-5-氧代-5,8-二氢-吡啶(2,3-d)嘧啶-6-羧酸，其中一些是新的化合物，通过将相应的嘧啶与氨基酯缩合，环化，卤代，脱卤化和皂化等过程制备而成。

  公开号：

  US04129737A1

文献信息

• [EN] PHARMACEUTICALLY ACTIVE SULFONAMIDE DERIVATIVES<br/>[FR] DERIVES SULFONAMIDES ACTIFS SUR LE PLAN PHARMACOLOGIQUE
  申请人：APPLIED RESEARCH SYSTEMS

  公开号：WO2001023378A1

  公开（公告）日：2001-04-05

  The present invention is related to sulfonamide derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. The compounds of formula (I) according to the present invention being suitable pharmaceutical agents are those wherein Ar?1 and Ar2¿ are independently from each other substituted or unsubstituted aryl or heteroaryl groups, X is O or S, preferably O; R1 is hydrogen or a C¿1?-C6-alkyl group, or R?1¿ forms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar1; n is an integer from 0 to 5, preferably between 1-3 and most preferred 1; Y within formula (I) is an unsubstituted or a substituted 4-12-membered saturated cyclic or bicyclic alkyl containing at least one nitrogen atom, whereby one nitrogen atom within said ring is forming a bond with the sulfonyl group of formula (I) thus providing a sulfonamide.

  本发明涉及公式（I）的磺酰胺衍生物，特别是作为药物活性化合物的用途，以及包含这种磺酰胺衍生物的制药配方。所述的磺酰胺衍生物是JNK通路的有效调节因子，特别是JNK 2和3的有效且选择性抑制剂。本发明还涉及新的磺酰胺衍生物以及其制备方法。根据本发明的公式（I）化合物适合作为药物代理，其中Ar?1和Ar2¿是独立于彼此的取代或未取代的芳基或杂环芳基基团，X为O或S，优选为O; R1是氢或C¿1?-C6烷基，或R?1¿与Ar1形成取代或未取代的5-6成员饱和或不饱和环；n为0到5的整数，优选为1-3，最优选为1；公式（I）中的Y是未取代或取代的4-12成员饱和环或双环烷基，其中至少有一个氮原子，在该环内与公式（I）的磺酰基形成化学键，从而提供磺酰胺。
• 8-Alkyl-5-oxo-5,8-dihydro-pyrido(2,3-d)pyrimidine-6-carboxylic acids and
  申请人：Laboratoire Roger Bellon

  公开号：US03950338A1

  公开（公告）日：1976-04-13

  Valuable antibacterial 8-alkyl-5-oxo-5,8-dihydro-pyrido(2,3-d)pyrimidine-6-carboxylic acids, some of which are new compounds, are made from corresponding pyrimidines by a process involving condensation with an amino-ester, cyclization, halogenation, dehydrohalogenation, and saponification.

  有价值的抗菌剂8-烷基-5-氧代-5,8-二氢吡啶并[2,3-d]嘧啶-6-羧酸，其中一些是新化合物，通过一种包括与氨基酯缩合，环化，卤代，脱卤化和皂化的过程从相应的嘧啶制备而成。
• 8-Alkyl-5-oxo-5,8-dihydro-pyrido(2,3-d)pyrimidine-6-carboxylic acids for
  申请人：Laboratoire Roger Bellow

  公开号：US04034094A1

  公开（公告）日：1977-07-05

  Valuable antibacterial 8-alkyl-5-oxo-5,8-dihydro-pyrido(2,3-d)pyrimidine-6-carboxylic acids, some of which are new compounds, are made from corresponding pyrimidines by a process involving condensation with an amino-ester, cyclization, halogenation, dehydrohalogenation, and saponification.

  有价值的抗菌8-烷基-5-氧代-5,8-二氢-吡啶[2,3-d]嘧啶-6-羧酸，其中一些是新化合物，通过将相应的嘧啶与氨基酯缩合，环化，卤代反应，脱卤化和皂化的过程制成。
• PHARMACEUTICALLY ACTIVE SULFONAMIDE DERIVATIVES
  申请人：Applied Research Systems ARS Holding N.V.

  公开号：EP1218374A1

  公开（公告）日：2002-07-03
• US3950338A
  申请人：——

  公开号：US3950338A

  公开（公告）日：1976-04-13