3t-(5-chloro-[2]furyl)-acrylic acid | 111252-98-3

• 分子结构分类: 有机化合物 - 有机卤素化合物 - 芳基卤化物
• 英文名称: 3t-(5-chloro-[2]furyl)-acrylic acid
• 英文别名: 3t-(5-Chlor-[2]furyl)-acrylsaeure；3-(5-Chloro-2-furyl)acrylic acid；(E)-3-(5-chlorofuran-2-yl)prop-2-enoic acid
• CAS: 111252-98-3
• 化学式: C₇H₅ClO₃
• 分子量: 172.568
• InChiKey: RVLDLKQBAJBUGU-DUXPYHPUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  50.4
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3t-(5-chloro-[2]furyl)-acrylic acid 在 三乙胺 作用下， 反应 3.5h， 生成 1-(4-amino-6,7-dimethoxy-quinazolin-2-yl)-4-[3-(5-chloro-furan-2-yl)-acryloyl]-piperazine
  参考文献：
  名称：

  Pyrimidine derivatives. 4. Synthesis and antihypertensive activity of 4-amino-2-(4-cinnamoylpiperazino)-6,7-dimethoxyquinazoline derivatives

  摘要：

  A series of 30 4-amino-2-(4-cinnamoylpiperazino)-6,7-dimethoxyquinazoline derivatives was prepared and tested for their ability to reduce blood pressure in conscious, spontaneously hypertensive rates (SHR). A number of these compounds, notably 4-amino-2-(4-cinnamoylpiperazino)-6,7-dimethoxyquinazolines 3a (R1 = H; R2 = Ph), 3j (R1 = H; R2 = 4-EtOPh), and 5a (R1 = H; R2 = 2-furyl), showed activity at oral doses of 0.3-10 mg/kg. The effects of the 4-substituents of the piperazino group on activity are discussed. Compounds 3a, 3j, and 5a were effective in renal hypertensive rats at oral doses of 3 and 10 mg/kg and showed alpha-adrenoceptor blocking effects in isolated aortas of rats. A 5-day consecutive oral administration of 3a and 3j in SHR did not lead to development of tolerance.

  DOI：

  10.1021/jm00357a016
• 作为产物：
  描述：

  5-氯-2-糠酸 在 吡啶 、 Pd-BaSO₄ 、 氯化亚砜 、 xylene 、 苯 作用下， 生成 3t-(5-chloro-[2]furyl)-acrylic acid
  参考文献：
  名称：

  Okuzumi, Nippon Kagaku Zasshi, 1958, vol. 79, p. 1366,1369

  摘要：

  DOI：

文献信息

• Nasarowa; Pimenowa, Zhurnal Obshchei Khimii, 1957, vol. 27, p. 2842,2843; engl. Ausg. S. 2879
  作者：Nasarowa、Pimenowa

  DOI：——

  日期：——
• Friedl, Zdenek; Boehm, Stanislav; Goljer, Igor, Collection of Czechoslovak Chemical Communications, 1987, vol. 52, # 2, p. 409 - 424
  作者：Friedl, Zdenek、Boehm, Stanislav、Goljer, Igor、Piklerova, Anna、Poorova, Daniela、et al

  DOI：——

  日期：——
• SEKIYA, TETSUO;HIRANUMA, HIDETOSHI;HATA, SHUNSUKE;MIZOGAMI, SUSUMU;HANAZU+, J. MED. CHEM., 1983, 26, N 3, 411-416
  作者：SEKIYA, TETSUO、HIRANUMA, HIDETOSHI、HATA, SHUNSUKE、MIZOGAMI, SUSUMU、HANAZU+

  DOI：——

  日期：——
• Pyrimidine derivatives. 4. Synthesis and antihypertensive activity of 4-amino-2-(4-cinnamoylpiperazino)-6,7-dimethoxyquinazoline derivatives
  作者：Tetsuo Sekiya、Hidetoshi Hiranuma、Shunsuke Hata、Susumu Mizogami、Mitsuo Hanazuka、Shunichi Yamada

  DOI：10.1021/jm00357a016

  日期：1983.3

  A series of 30 4-amino-2-(4-cinnamoylpiperazino)-6,7-dimethoxyquinazoline derivatives was prepared and tested for their ability to reduce blood pressure in conscious, spontaneously hypertensive rates (SHR). A number of these compounds, notably 4-amino-2-(4-cinnamoylpiperazino)-6,7-dimethoxyquinazolines 3a (R1 = H; R2 = Ph), 3j (R1 = H; R2 = 4-EtOPh), and 5a (R1 = H; R2 = 2-furyl), showed activity at oral doses of 0.3-10 mg/kg. The effects of the 4-substituents of the piperazino group on activity are discussed. Compounds 3a, 3j, and 5a were effective in renal hypertensive rats at oral doses of 3 and 10 mg/kg and showed alpha-adrenoceptor blocking effects in isolated aortas of rats. A 5-day consecutive oral administration of 3a and 3j in SHR did not lead to development of tolerance.
• Okuzumi, Nippon Kagaku Zasshi, 1958, vol. 79, p. 1366,1369
  作者：Okuzumi

  DOI：——

  日期：——