| Negishi偶联反应在沙坦类药物联苯基合成中的应用 |
| |
| 引用本文： | 王晓东,黄素萍,时敏,郝卫强,陈强. Negishi偶联反应在沙坦类药物联苯基合成中的应用[J]. 药学进展, 2012, 36(5): 227-230 |
| |
| 作者姓名： | 王晓东 黄素萍 时敏 郝卫强 陈强 |
| |
| 作者单位： | 1. 常州四药制药有限公司,江苏 常州,213004
2. 南京大学常州高新技术研究院,江苏 常州,213164 |
| |
| 摘 要： | 目的：探索沙坦类药物新的合成方法,简化其合成步骤。方法：以价廉易得的化合物为原料,合成中间体N-戊酰基-N-[（4-溴）-苯甲基]-L-缬氨酸甲酯和5-苯基-1-三苯甲基四氮唑,并经Negishi偶联合成目标化合物缬沙坦。结果与结论：目标物的化学结构经核磁共振氢谱、碳谱、质谱、红外光谱和元素分析确证。合成工艺的总收率为55%。
|
| 关 键 词： | 缬沙坦 Negishi偶联反应 药物合成 |
Application of Negishi Coupling Reaction in the Synthesis of Biphenyl Group in Sartans |
| |
| WANG Xiao-dong , HUANG Su-ping , SHI Min , HAO Wei-qiang , CHEN Qiang. Application of Negishi Coupling Reaction in the Synthesis of Biphenyl Group in Sartans[J]. Progress in Pharmaceutical Sciences, 2012, 36(5): 227-230 |
| |
| Authors: | WANG Xiao-dong HUANG Su-ping SHI Min HAO Wei-qiang CHEN Qiang |
| |
| Affiliation: | 1.Changzhou Siyao Pharmaceuticals Co.,Ltd.,Changzhou 213004,China;2.Changzhou High-Tech Research Institute of Nanjing University,Changzhou 213164,China) |
| |
| Abstract: | Objective:To simplify the synthetic procedure of valsartan.Methods:The target product valsartan was synthesized by Negishi coupling reaction of intermediates methyl N-(4-bromobenzyl)-N-pentanayl-L-valinate and 5-phenyl-1-trityl-1H-tetrazole which were prepared from the cheap and accessible starting materials.Results and Conclusion:The chemical structure of target product was confirmed by 1H-NMR,13C-NMR,MS,IR and EI.The overall yield of target product was 55%. |
| |
| Keywords: | valsartan Negishi coupling reaction drug synthesis |
| 本文献已被 CNKI 维普 万方数据 等数据库收录！ |
|
