| 法可林中间体——7,8-二氨基吩嗪-2-磺酸的合成 |
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| 引用本文： | 曹甲臣,陈仁财,韩静.法可林中间体——7,8-二氨基吩嗪-2-磺酸的合成[J].合成化学,2016(5). |
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| 作者姓名： | 曹甲臣 陈仁财 韩静 |
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| 作者单位： | 沈阳药科大学制药工程学院,辽宁沈阳,110016 |
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| 摘 要： | 研究了3条合成法可林中间体7,8-二氨基吩嗪-2-磺酸(1)]的工艺路线(路线A~C)。结果表明:路线C为最优反应条件,即以邻苯二胺为起始原料,先用浓硫酸磺化,再经保护-氧化反应,最后脱除保护基合成了1,总收率62.01%,其结构经~1H NMR,~(13)C NMR和ESI-MS确证。
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| 关 键 词： | 法可林 中间体合成 7 8-二氨基吩嗪-2-磺酸 药物合成 工艺优化 |
Synthesis of 7,8-Diaminophenazine-2-sulfonic Acid,An Intermediate for Phacolysin |
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| Abstract: | Three routes(route A~C) of synthesizing phacolysin intermediate , 7,8-diaminophenazine-2-sulfonic acid(1), were investigated.The results showed that route C was the best method .1 was synthesized by sulfuric acid sulfonation , protection-oxidation and deprotection , respectively .The total yield was 62.01%.The structure was confirmed by 1 H NMR, 13 C NMR and ESI-MS. |
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| Keywords: | phacolysin intermediate synthesis 7 8-diaminophenazine-2-sulfoniacid acid drug syn-thesis process improvement |
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