| 6-(4-氨基苯基)-5-甲基-4,5-二氢-3(2H)-哒嗪酮的拆分及左西孟旦的合成 |
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| 引用本文： | 张丽娟,宋宏锐,王玉玲,宋爱华.6-(4-氨基苯基)-5-甲基-4,5-二氢-3(2H)-哒嗪酮的拆分及左西孟旦的合成[J].沈阳药科大学学报,2004,21(1):22-23. |
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| 作者姓名： | 张丽娟 宋宏锐 王玉玲 宋爱华 |
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| 作者单位： | 1. 沈阳药科大学制药工程学院,辽宁,沈阳,110016
2. 沈阳药科大学药学院,辽宁,沈阳,110016 |
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| 摘 要： | 目的合成治疗急性心衰新药左西孟旦。方法以乙酰苯胺为原料 ,经Friedel Crafts酰化反应、Mannich反应、氰化、水解、环合反应制得 6 (4 氨基苯基 ) 5 甲基 4,5 二氢 3 (2H) 哒嗪酮 ,并对该化合物的拆分条件进行了探索和优化。拆分后的左旋体经两步反应制得左西孟旦。结果与结论拆分一步收率较文献大大提高 ,达 5 4 9%。合成左西孟旦总收率为 1 8 4%。
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| 关 键 词： | 左西孟旦 合成 拆分 |
| 文章编号： | 1006-2858(2004)01-0022-02 |
| 修稿时间： | 2003年5月22日 |
Resolution of 6-(4-aminophenyl)-5-methyl-4,5-dihydropyridazin-3(2H)-one and synthesis of levosimendan |
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| ZHANG Li-juan,SONG Hong-rui,WANG Yu-ling,SONG Ai-hua.Resolution of 6-(4-aminophenyl)-5-methyl-4,5-dihydropyridazin-3(2H)-one and synthesis of levosimendan[J].Journal of Shenyang Pharmaceutical University,2004,21(1):22-23. |
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| Authors: | ZHANG Li-juan SONG Hong-rui WANG Yu-ling SONG Ai-hua |
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| Abstract: | Objective To prepare levosimendan,an acute heart-failure agent.Methods 6-(4-aminophenyl)-4,5-dihydropyridazin-3(2 H )-one was prepared from acetanilide through the Friedel-Crafts acetylation,Mannich reaction,cyanogenation,hydrolysis,cyclization,and its resolution was studied,and levosimendan was prepared from levo-isomer from the resolution through two reactions.Results and Conclusions Levosimendan was synthesized in an overall yield of 18.4%.The resolution technique of the key intermediate,6-(4-aminophenyl)-4,5-dihydropyridazin-3(2 H )-one,is improved with a better yield than that in the literature. |
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| Keywords: | levosimendan synthesis resolution |
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