| 高选择性N-单甲基化芳香胺的合成 |
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| 引用本文： | 彭以元a 刘汉亮a 唐敏a CAI,Lisheng PIKE,Victor.高选择性N-单甲基化芳香胺的合成[J].中国化学,2009,27(7):1339-1344. |
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| 作者姓名： | 彭以元a 刘汉亮a 唐敏a CAI Lisheng PIKE Victor |
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| 作者单位： | a江西省绿色化学重点实验室，江西师范大学化学系， 江西南昌（330022） ;bPET Radiopharmaceutical Sciences Section, Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892, USA ; |
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| 摘 要： | 本文报道了一种高效专一性合成N-单甲基芳胺的方法。芳胺先与醋酐反应生成乙酰胺，再与碘甲烷在氢化钠作用下反应生成相应的N-甲基乙酰芳胺。在乙二醇中用酸水解高产率得到相应的N-单甲基芳胺。并将该方法用于药物中间体的合成。
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| 关 键 词： | N-甲基化反应 芳香胺 N-甲基乙酰芳胺 N-单甲基芳胺 酸水解 乙二醇 |
| 收稿时间： | 2008-8-1 |
| 修稿时间： | 2008-11-27 |
Highly Efficient N‐Monomethylation of Primary Aryl Amines |
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| Yiyuan PENG,Hanliang LIU,Min TANG,Lisheng CAI,Victor PIKE.Highly Efficient N‐Monomethylation of Primary Aryl Amines[J].Chinese Journal of Chemistry,2009,27(7):1339-1344. |
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| Authors: | Yiyuan PENG Hanliang LIU Min TANG Lisheng CAI Victor PIKE |
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| Institution: | 1. Jiangxi Key Laboratory of Green Chemistry, Department of Chemistry, Jiangxi Normal University, Nanchang, Jiangxi 330027, China;2. Positron Emission Tomography Radiopharmaceutical Sciences Section, Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892, USA |
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| Abstract: | A highly efficient method for specific synthesis of N‐monomethylarylamines is presented. Anilines were treated with acetic anhydride and triethylamine in dry CH2Cl2 to give the corresponding acetamides. The subsequent N‐monomethylation of acetyl aryl amines with methyl iodide and NaH in THF introduced methyl group. Acid hydrolysis of the N‐methyl acetanilides in ethylene glycol generated the corresponding N‐methyl‐N‐aryl amines in high yields. This method was also used to synthesize (E)‐2‐bromo‐5‐(4‐methylaminostyryl)pyridine that may be useful as an amyloid imaging agent for Alzheimer's disease. |
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| Keywords: | N‐monomethylation N‐methylaniline N‐methyl acetanilide methyl iodide ethylene glycol |
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