| 4-(4-氨基苯基)-3-吗啉酮的合成 |
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| 引用本文： | 罗玲艳,申东升,周宗洲,谭诚,黄英堂. 4-(4-氨基苯基)-3-吗啉酮的合成[J]. 中国医药工业杂志, 2011, 42(2) |
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| 作者姓名： | 罗玲艳 申东升 周宗洲 谭诚 黄英堂 |
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| 作者单位： | 广东药学院医药化工学院,广东广州,510006 |
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| 摘 要： | 用两种方法制得抗凝剂利伐沙班的中间体4-(4-氨基苯基)-3-吗啉酮(1):①溴苯相继与乙醇胺、氯乙酰氯反应得4-苯基吗啉酮,再经硝化、还原生成1,总收率约32%;②溴苯先硝化,再与乙醇胺反应得到2-(4-硝基苯胺基)乙醇,再经氯乙酰氯闭环、还原反应制得1,总收率约47%.
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| 关 键 词： | 4-(4-氨基苯基)-3-吗啉酮 利伐沙班 抗凝药 中间体 合成 |
Synthesis of 4- (4-Aminophenyl) -3-morpholinone |
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| LUO Lingyan,SHEN Dongsheng,ZHOU Zongzhou,TAN Cheng,HUANG Yingtang. Synthesis of 4- (4-Aminophenyl) -3-morpholinone[J]. , 2011, 42(2) |
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| Authors: | LUO Lingyan SHEN Dongsheng ZHOU Zongzhou TAN Cheng HUANG Yingtang |
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| Affiliation: | LUO Lingyan,SHEN Dongsheng~*,ZHOU Zongzhou,TAN Cheng,HUANG Yingtang (School of Chemistry and Chemical Engineering,Guangdong Pharmaceutical University,Guangzhou 510006) |
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| Abstract: | 4-(4-Aminophenyl)-3-morpholinone is the key intermediate of anticoagulant rivaroxaban.Two synthetic routes were achieved from bromobenzene.One is that bromobenzene reacted with 2-aminoethanol to give 2-anilinoethanol,which was subjected to cyclization with chloroacetyl chloride,followed by nitration and reduction with an overall yield of about 32%.The other is that bromobenzene underwent a sequence of reactions of nitration, N-arylation,acylation,cyclization and reduction with an overall yield of about 47%. |
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| Keywords: | 4-(4-aminophenyl)-3-morpholinone rivaroxaban anticoagulant intermediate synthesis |
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