| 盐酸喹那普利的合成 |
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| 引用本文： | 孙平华,姚志红,于荣敏,陈卫民,孙铁民. 盐酸喹那普利的合成[J]. 中国新药杂志, 2006, 15(22): 1945-1947 |
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| 作者姓名： | 孙平华 姚志红 于荣敏 陈卫民 孙铁民 |
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| 作者单位： | 1. 暨南大学药学院,广州,510632
2. 沈阳药科大学制药工程学院,沈阳,110015 |
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| 摘 要： | 目的：合成强效、高特异性血管紧张素转化酶（ACE）抑制剂盐酸喹那普利。方法：以β-苯甲酰丙烯酸乙酯和L-丙氨酸为原料，经加成、脱苄、环合、还原制得盐酸喹那普利，并通过改变反应温度、反应物间的投料比和后处理对其合成工艺进行改进。结果和结论：得到的产品经IR，^1H-NMR，MS和元素分析，证明是盐酸喹那普利。本合成工艺的收率为25．3％。
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| 关 键 词： | 喹那普利 血管紧张素转化酶抑制剂 药物合成 |
| 文章编号： | 1003-3734（2006）22-1945-03 |
| 收稿时间： | 2006-03-30 |
| 修稿时间： | 2006-03-30 |
Improved preparation of quinapril |
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| SUN Ping-hua,YAO Zhi-hong,YU Rong-min,CHEN Wei-min,SUN Tie-min. Improved preparation of quinapril[J]. Chinese Journal of New Drugs, 2006, 15(22): 1945-1947 |
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| Authors: | SUN Ping-hua YAO Zhi-hong YU Rong-min CHEN Wei-min SUN Tie-min |
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| Affiliation: | 1 Faculty of Pharmacy, Jinan University, Guangzhou 510632, China; 2 School of Pharmaceutic Engineering, Shenyang Pharmaceutical University, Shen yang 110016, China |
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| Abstract: | Objective:To synthesize ACE inhibitor quinapril.Methods:Starting from 4-oxo-4- phenyl-but-2-enoic acid ethyl ester,quinapril was prepared via several steps including addition,debenzy- lation,cyclization and reduction.The reaction temperature,ratio of raw reactive agents used and post- treatment of the synthetic procedure were optimized.Results and Conclusion:The chemical structure of quinapril was confirmed by IR,MS and ~1H-NMR.The overall yield was 25.6%.The modified synthetic procedure for quinapril was attainable. |
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| Keywords: | quinapril ACE inhibitor drug synthesis |
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