4-(2-chloro-4-fluorophenyl)-1,3-thiazol-2-amine | 145029-84-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-(2-chloro-4-fluorophenyl)-1,3-thiazol-2-amine
• CAS: 145029-84-1
• 化学式: C₉H₆ClFN₂S
• mdl: MFCD07366420
• 分子量: 228.677
• InChiKey: YKUHOXMBKIGRFZ-UHFFFAOYSA-N

物化性质

• 沸点：
  361.2±27.0 °C(Predicted)
• 密度：
  1.467±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  67.2
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  4-(2-chloro-4-fluorophenyl)-1,3-thiazol-2-amine 以 1,4-二氧六环 、 溶剂黄146 为溶剂， 反应 7.0h， 生成 N-[4-(2-chloro-4-fluorophenyl)-thiazol-2-yl]-2-diethylamino acetamide
  参考文献：
  名称：

  Synthesis and local anaesthetic activities of 2-aminothiazole/thiadiazole analogues of lidocaine

  摘要：

  Various 2-aminothiazole and 2-aminothiadiazole derivatives viz N-[4-(2-Chloro-4-fluoro-phenyl)-thiazol-2-yl]-2-substituted acetamides (3a, 4a, 5a) and N-[5-(4-substituted aryl)-[1,3,4]thiadiazol-2-yl]-2-acetamides (3b, 3c, 4b, 4c, 5b, 5c) were synthesized from their corresponding properly substituted 2-aminothiazoles and 2-aminothiadiazoles. Structures of all the newly synthesized compounds were established by analytical and spectral data. Synthesized compounds were screened for their local anaesthetic activity using the rat sciatic nerve model.Various 2-aminothiazole and 2-aminothiadiazole derivatives viz N-[4-(2-Chloro-4-fluoro-phenyl)-thiazol-2-yl]-2-substituted acetamides (3a, 4a, 5a) and N-[5-(4-substituted aryl)-[1,3,4]thiadiazol-2-yl]-2-acetamides (3b, 3c, 4b, 4c, 5b, 5c) were synthesized from their corresponding properly substituted 2-aminothiazoles and 2-aminothiadiazoles. Structures of all the newly synthesized compounds were established by analytical and spectral data. Synthesized compounds were screened for their local anaesthetic activity using the rat sciatic nerve model.

  DOI：

  10.1007/s00044-011-9659-4

文献信息

• QUINAZOLINEDIONE DERIVATIVES AS TRPA1 MODULATORS
  申请人：Muthuppalniappan Meyyappan

  公开号：US20090325987A1

  公开（公告）日：2009-12-31

  The present invention provides Quinazolinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.

  本发明提供了喹唑啉二酮衍生物作为TRPA（瞬时受体电位亚家族A）调节剂。具体来说，本文描述的化合物可用于治疗或预防由TRPA1（瞬时受体电位亚家族A，成员1）调节的疾病、病况和/或疾病。本文还提供了制备本文描述的化合物的方法、用于合成的中间体、药物组合物以及治疗或预防由TRPA1调节的疾病、病况和/或疾病的方法。
• Synthesis and Pesticidal Activities of O,O- Dialkyl-N-[(4-aryl)-2-thiazolyl] Phosphoramidothioates
  作者：Renuka Jain、Satish C. Jain、Praveen Kumar Goyal、Shipra Vajpei

  DOI：10.1080/10426500701512208

  日期：2007.9.13

  Several fluorine-containing O,O-dialkyl-N-[(4-aryl)-2-thiazolyl] phosphoramidothoiates were synthesized as possible antifungal and insecticidal agents by treating appropriate 2-amino-4-aryl-thiazoles with O,O-dialkyl phosphorochloridothioates. The latter were obtained by the reaction of dry alcohol on thiophosphoryl chloride in the presence of sodium metal. Some of the synthesized compounds exhibited

  通过用 O,O-二烷基处理适当的 2-氨基-4-芳基-噻唑，合成了几种含氟 O,O-二烷基-N-[(4-芳基)-2-噻唑基] 氨基硫代磷酸酯作为可能的抗真菌和杀虫剂硫代氯代磷酸酯。后者是在金属钠存在下通过无水醇与硫代磷酰氯反应获得的。一些合成的化合物对曲霉属物种表现出显着的抗真菌活性。在杀虫活性方面，具有甲基和氟的化合物表现出增强的效果。还注意到活性随着烷基的大小和支化而增加。
• US7951814B2
  申请人：——

  公开号：US7951814B2

  公开（公告）日：2011-05-31
• Synthesis and local anaesthetic activities of 2-aminothiazole/thiadiazole analogues of lidocaine
  作者：Naveen P. Badiger、Ashraf Khan、M. B. Kalashetti、I. M. Khazi

  DOI：10.1007/s00044-011-9659-4

  日期：2012.8

  Various 2-aminothiazole and 2-aminothiadiazole derivatives viz N-[4-(2-Chloro-4-fluoro-phenyl)-thiazol-2-yl]-2-substituted acetamides (3a, 4a, 5a) and N-[5-(4-substituted aryl)-[1,3,4]thiadiazol-2-yl]-2-acetamides (3b, 3c, 4b, 4c, 5b, 5c) were synthesized from their corresponding properly substituted 2-aminothiazoles and 2-aminothiadiazoles. Structures of all the newly synthesized compounds were established by analytical and spectral data. Synthesized compounds were screened for their local anaesthetic activity using the rat sciatic nerve model.Various 2-aminothiazole and 2-aminothiadiazole derivatives viz N-[4-(2-Chloro-4-fluoro-phenyl)-thiazol-2-yl]-2-substituted acetamides (3a, 4a, 5a) and N-[5-(4-substituted aryl)-[1,3,4]thiadiazol-2-yl]-2-acetamides (3b, 3c, 4b, 4c, 5b, 5c) were synthesized from their corresponding properly substituted 2-aminothiazoles and 2-aminothiadiazoles. Structures of all the newly synthesized compounds were established by analytical and spectral data. Synthesized compounds were screened for their local anaesthetic activity using the rat sciatic nerve model.