| An Efficient Synthesis of Selective Human NR2A Antagonist NVP-AAM077 |
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| 引用本文： | 李纲琴 苏为科 姚祝军. An Efficient Synthesis of Selective Human NR2A Antagonist NVP-AAM077[J]. 中国化学, 2006, 24(12): 1784-1787. DOI: 10.1002/cjoc.200690333 |
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| 作者姓名： | 李纲琴 苏为科 姚祝军 |
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| 作者单位： | [1]State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China [2]College of Pharmaceutical Sciences, Zhejiang University of Technology, tIangzhou, Zhejiang 310014, China |
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| 基金项目： | Project supported by the Natural Science Foundation of China （Nos. 20425205, 20321202）, Chinese Academy of Sciences （No. KGCX2-SW-209） and Shanghai Municipal Commission of Science and Technology （No. 04DZ14901）. |
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| 摘 要： | A short and efficient synthesis of the selective human N-methyl-D-aspartate （NMDA） receptor 2A （NR2A） antagonist NVP-AAM077 is described. The target was achieved in 8 steps and in 54% overall yield from the commercially available chemical 3-methylbenzene-1,2-diamine. A NaIO4/DMF-based oxidation of the bromide to corresponding aldehyde and an addition of phosphinic acid ester to the aldimine successfully served as the key steps.
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| 关 键 词： | N-甲基-D-天门冬胺酸酯受体2A 拮抗剂 NVP-AAM077 合成 氨基磷酸 药物 离子通道 |
| 收稿时间： | 2006-03-09 |
| 修稿时间： | 2006-03-092006-07-24 |
An Efficient Synthesis of Selective Human NR2A Antagonist NVP-AAM077 |
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| LI Gang-Qin, SU Wei-Ke, YAO Zhu-Jun. An Efficient Synthesis of Selective Human NR2A Antagonist NVP-AAM077[J]. Chinese Journal of Chemistry, 2006, 24(12): 1784-1787. DOI: 10.1002/cjoc.200690333 |
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| Authors: | LI Gang-Qin SU Wei-Ke YAO Zhu-Jun |
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| Affiliation: | 1. State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China ;2. College of Pharmaceutical Sciences, Zhejiang University of Technology, tIangzhou, Zhejiang 310014, China |
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| Abstract: | A short and efficient synthesis of the selective human N-methyl-D-aspartate(NMDA)receptor 2A (NR2A) an- tagonist NVP-AAM077 is described.The target was achieved in 8 steps and in 54% overall yield from the commer- cially available chemical 3-methylbenzene-1,2-diamine.A NaIO_4/DMF-based oxidation of the bromide to corre- sponding aldehyde and an addition of phosphinic acid ester to the aldimine successfully served as the key steps. |
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| Keywords: | NMDA receptor 2A antagonist NVP-AAM077 synthesis amino phosphonic acid |
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