| 2-氨基烟酸的合成 |
| |
| 引用本文： | 苏策,张凯明,贺俊华. 2-氨基烟酸的合成[J]. 化工学报, 2011, 62(2): 580-583 |
| |
| 作者姓名： | 苏策 张凯明 贺俊华 |
| |
| 作者单位： | 兰州理工大学石油化工学院 |
| |
| 摘 要： | 2-氨基烟酸(2-aminonicotinic acid),化学名2-氨基吡啶-3-羧酸,作为中间体在药物合成中有着广泛的应用[1-5].如Alexandros等[5]以2-氨基烟酸为原料合成抗菌、抗炎药物萘啶酮.因此,开发其简便、高效、操作安全的合成工艺,具有极其重要的意义.
|
| 关 键 词： | 2-氨基烟酸 喹啉 Hofmann降解反应 |
Synthesis of 2-aminonicotinic acid |
| |
| SU Ce,ZHANG Kaiming,HE Junhua. Synthesis of 2-aminonicotinic acid[J]. Journal of Chemical Industry and Engineering(China), 2011, 62(2): 580-583 |
| |
| Authors: | SU Ce ZHANG Kaiming HE Junhua |
| |
| Abstract: | 2-Aminonicotinic acid is an important synthetic intermediate of many drugs.A novel four-step synthesis method for preparing 2-aminonicotinic acid from quinoline is developed.The overall yield of 2-aminonicotinic acid is up to 29% based on quinoline.The oxidation of quinoline gives 2,3-pyridine dicarboxylic acid, and after intramolecular dehydration mediated by acetic anhydride, 2,3-pyridine dicarboxylic anhydride is obtained.Then, this anhydride is subjected to ammonolysis followed by Hofmann degradation reaction to introduce C(2）amino group,completing the synthesis of target molecule 2-aminonicotinic acid.NaClO3-H2SO4-CuSO4 is prominently superior to KMnO4 as oxidant to quinoline, so that the yield is improved to 65.2%.The conditions of anhydride ammonolysis and Hofmann degradation were also optimized.The developed synthetic technologies are suitable for large-scale preparation, and the highlights include low cost and availability of starting material, safe operation, simple separation and purification, and high purity of final product.The target product with 98% HPLC purity is characterized by 1H NMR and IR. |
| |
| Keywords: | |
| 本文献已被 万方数据 等数据库收录！ |
| 点击此处可从《化工学报》浏览原始摘要信息 |
|
点击此处可从《化工学报》下载免费的PDF全文 |
|
