An Efficient Synthesis of Selective Human NR2A Antagonist NVP-AAM077  

作　　者：李纲琴 苏为科 姚祝军 

机构地区：[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

出　　处：《Chinese Journal of Chemistry》2006年第12期1784-1787,共4页中国化学（英文版）

基　　金：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）.

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.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.

关 键 词：NMDA receptor 2A ANTAGONIST NVP-AAM077 SYNTHESIS amino phosphonic acid 

分 类 号：R96[医药卫生—药理学]