| 阿哌沙班的合成工艺改进 |
| |
| 引用本文： | 王鹏,林丽红. 阿哌沙班的合成工艺改进[J]. 中国现代应用药学, 2019, 36(14): 1783-1786 |
| |
| 作者姓名： | 王鹏 林丽红 |
| |
| 作者单位： | 浙江华海药业股份有限公司, 浙江 台州 317016,浙江华海药业股份有限公司, 浙江 台州 317016 |
| |
| 摘 要： | 目的 改进阿哌沙班的合成工艺。方法 以3-吗啡啉-1-（4-硝基苯基）-5,6-二氢吡啶-2（1H）-酮（2）为起始原料,经缩合,氨化和"一锅法"还原和环合反应,得到阿哌沙班（1）。结果 中间体和目标化合物的结构经1H-NMR、13C-NMR、高分辨质谱确证,3步合成总收率为50.2%。结论 改进后的工艺适合工业化生产。
|
| 关 键 词： | 阿哌沙班 合成 优化 |
| 收稿时间： | 2018-07-10 |
Improvement on Synthesis Process of Apixaban |
| |
| WANG Peng and LIN Lihong. Improvement on Synthesis Process of Apixaban[J]. The Chinese Journal of Modern Applied Pharmacy, 2019, 36(14): 1783-1786 |
| |
| Authors: | WANG Peng and LIN Lihong |
| |
| Affiliation: | Zhejiang Huahai Pharmaceutical Co., Ltd., Taizhou 317016, China and Zhejiang Huahai Pharmaceutical Co., Ltd., Taizhou 317016, China |
| |
| Abstract: | OBJECTIVE To improve the synthesis process of apixaban. METHODS Apixaban(1) was synthesized by using 3-morpholino-1-(4-nitrophenyl)-5,6-dihydropyridin-2(1H)-one(2) as the starting material, via condensation, aminolysis and "one-pot" reaction inculding reduction and cyclization. RESULTS The structures of intermediates and target molecule were confirmed by 1H-NMR, 13C-NMR and HRMS. The overall yield was 50.2% over 3 steps. CONCLUSION The improved process is suitable for industrial scaling-up. |
| |
| Keywords: | apixaban synthesis optimization |
|
| 点击此处可从《中国现代应用药学》浏览原始摘要信息 |
|
点击此处可从《中国现代应用药学》下载全文 |
|
