ethyl 3--4-(3-furyl)-4-oxobutyrate | 88352-61-8

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: ethyl 3--4-(3-furyl)-4-oxobutyrate
• 英文别名: ethyl 3-(4-chlorobenzoylamino)-3-(3-furylcarbonyl)propionate；ethyl 3-(4-chlorobenzoylamino)-3-(furan-3-ylcarbonyl)propionate；ethyl 3-[(4-chlorobenzoyl)amino]-4-(furan-3-yl)-4-oxobutanoate
• CAS: 88352-61-8
• 化学式: C₁₇H₁₆ClNO₅
• 分子量: 349.771
• InChiKey: RVDXYLOLHLYGQY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  24
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  85.6
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  ethyl 3--4-(3-furyl)-4-oxobutyrate 在 三氯氧磷 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 8.0h， 以86%的产率得到ethyl 2-[2-(4-chlorophenyl)-5-(furan-3-yl)-4-oxazolyl]acetate
  参考文献：
  名称：

  Synthesis of ethyl 2-(4-chlorophenyl)-5-(2-furyl)-4-oxazoleacetate, a hypolipidemic agent, and related compounds

  摘要：

  A series of 2-aryl and 2-alkyl derivatives of 5-furyl-4-oxazoleacetic acid and their homologues having alkyl groups at the alpha-position of the acids were synthesized and evaluated for their hypolipidemic activities in Sprague-Dawley rats. On the basis of the structure-activity relationships and subacute toxicities, ethyl 2-(4-chlorophenyl)-5-(2-furyl)-4-oxazoleacetate (35) was selected as a candidate compound for development. Compound 35 reduced serum cholesterol and triglyceride levels by 23% and 35%, respectively, at a dose of 0.05% in a diet in normal rats, and it was about 10 times more active in hereditary hyperlipidemic rats (THLR/1) than in normal rats. Compound 35 inhibited platelet aggregation in vitro and also normalized hyperaggregability of hyperlipidemic plasma platelet ex vivo.

  DOI：

  10.1021/jm00401a021
• 作为产物：
  描述：

  N-<(4-chlorobenzoyl)amino>methyl 3-furyl ketone 生成 ethyl 3--4-(3-furyl)-4-oxobutyrate
  参考文献：
  名称：

  摘要：

  DOI：

文献信息

• Furyloxazolylacetic acid derivatives and processes for preparing same
  申请人：Tanabe Seiyaku Co., Ltd.

  公开号：US04642313A1

  公开（公告）日：1987-02-10

  A furyloxazolylacetic acid derivative of the formula: ##STR1## wherein R.sup.1 is alkyl of one to 6 carbon atoms, cycloalkyl of 5 to 6 carbon atoms, phenyl or a substituted phenyl (said substituted phenyl being phenyl group substituted with one or two radicals selected from alkyl of one to 2 carbon atoms, alkoxy of one to 2 carbon atoms and halogen), and R.sup.2 is hydrogen or alkyl of one to 12 carbon atoms. The compound (I) is useful as a hypolipidemic agent.

  一种 furyloxazolylacetic 酸衍生物的化学式为：##STR1## 其中 R.sup.1 是1至6个碳原子的烷基，5至6个碳原子的环烷基，苯基或取代苯基（所述取代苯基是苯基，其上取代有一个或两个来自1至2个碳原子的烷基、1至2个碳原子的烷氧基和卤素的基团），而 R.sup.2 是氢或1至12个碳原子的烷基。该化合物（I）可用作降脂药剂。
• Furyloxazolylacetic acid derivative, processes for preparing same and pharmaceutical composition
  申请人：Tanabe Seiyaku Co., Ltd.

  公开号：EP0120270A2

  公开（公告）日：1984-10-03

  A furyloxazolylacetic acid derivative of the formula: wherein R' is lower alkyl, R2 is hydrogen atom or lower alkyl, R3 is hydrogen atom or lower alkyl and ring A is phenyl or halogenophenyl, processes for preparing same and pharmaceutical compositions containing the new compounds, which are useful as a hypolipidemic agent are disclosed.

  一种式中R'为低级烷基，R2为氢原子或低级烷基，R3为氢原子或低级烷基，环A为苯基或卤素苯基的呋喃恶唑乙酸衍生物，其制备方法以及含有该衍生物的药物组合物： 其中R'为低级烷基，R2为氢原子或低级烷基，R3为氢原子或低级烷基，环A为苯基或卤代苯基，公开了制备这些新化合物的工艺和含有这些新化合物的药物组合物，它们可用作降血脂剂。
• MORIYA, TAMON;SEKI, MASAHIKO;TAKABE, SEIICHI;MATSUMOTO, KAZUO;TAKASHIMA, +, J. MED. CHEM., 31,(1988) N 6, 1197-1204
  作者：MORIYA, TAMON、SEKI, MASAHIKO、TAKABE, SEIICHI、MATSUMOTO, KAZUO、TAKASHIMA, +

  DOI：——

  日期：——
• ——
  作者：MATSUMOTO KAZUO、 TAKASHIMA KOHKI

  DOI：——

  日期：——
• Furyloxazolylacetic acid derivatives, process for preparing same and pharmaceutical compositions containing same
  申请人：Tanabe Seiyaku Co., Ltd.

  公开号：EP0087782B1

  公开（公告）日：1986-05-21