| 1,4—二氢吡啶类钙拮抗剂的合成法研究——(Ⅰ)尼群地平改进合成工艺 |
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| 引用本文： | 陈芬儿,沈怡,李艳.1,4—二氢吡啶类钙拮抗剂的合成法研究——(Ⅰ)尼群地平改进合成工艺[J].武汉化工学院学报,1993(3). |
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| 作者姓名： | 陈芬儿 沈怡 李艳 |
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| 作者单位： | 武汉化工学院精细化工系
(陈芬儿，沈怡)，武汉化工学院精细化工系(李艳) |
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| 摘 要： | 间硝基亚苄基乙酰乙酸乙酯与3-氨基丁烯酸甲酯在原位形成的哌啶乙酸盐的催化下经Michael加成反应环合制得尼群地平。对关键中间体间硝基亚苄基乙酰乙酸乙酯的制备进行了改进。以间硝基苯甲醛计算,总收率93％。此法原料易得,反应条件温和,适合工业化生产。
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| 关 键 词： | 尼群地平 钙拮抗剂 Knoevenagel-Doebner缩合 环合 Michael加成 合成 |
Study on Synthesizing the Calcium Antagonist of 1, 4-Dihydropyridines ( I ) An Improved Process for Synthesis of Nitrendipine |
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| Chen Fener Shen Yi Li yan.Study on Synthesizing the Calcium Antagonist of 1, 4-Dihydropyridines ( I ) An Improved Process for Synthesis of Nitrendipine[J].Journal of Wuhan Institute of Chemical Technology,1993(3). |
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| Authors: | Chen Fener Shen Yi Li yan |
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| Affiliation: | Chen Fener Shen Yi Li yan |
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| Abstract: | Nitrendipine was synthesized from ethyl 3-nitrobenzy Lideneacetoacetate and methyl 3- aminocrotonate in the presence of piperidine acetate formed in situ via cyclising Michael reaction in about 93% overall yield from 3-nitrobenzaldehyde. The preparation of key intermediate ethyl 3-nitrobf nzylidene acetoacetate was improved. The mild reaction conditions, convenient work-up high overall yiled and purity were the advantages of this method. |
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| Keywords: | Nitrendipine Calcium antagonist Knoevenagel-Doebner condensation Cyclising Michael addition Synthesis |
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