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An Efficient Synthesis of Selective Human NR2A Antagonist NVP-AAM077
  • ISSN号：1001-604X
  • 期刊名称：《中国化学：英文版》
  • 时间：0
  • 分类：R96[医药卫生—药理学;医药卫生—药学]
  • 作者机构：[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
  • 相关基金：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）.
作者： 李纲琴[1,2], 苏为科[2], 姚祝军[1]
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, NMDA receptor 2A, antagonist, NVP-AAM077, synthesis, amino phosphonic acid
中文摘要：

选择人的 N-methyl-D-aspartate (NMDA ) 受体 2A (NR2A ) 的短、有效的合成对手 NVP-AAM077 被描述。目标从商业地可得到的化学 3-methylbenzene-1,2-diamine 在 8 步并且在 54% 全面产量被完成。当钥匙走，到相应的醛和到 aldimine 的 phosphinic 酸酉旨的增加的溴化物的 NaIO4/DMF-based 氧化成功地服务了。

英文摘要：

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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期刊信息
  • 《中国化学：英文版》
  • 主管单位:
  • 主办单位:中国化学会
  • 主编：
  • 地址：上海市枫林路354号中科院上海有机化学研究所
  • 邮编：200032
  • 邮箱：
  • 电话：021-54925243
  • 国际标准刊号：ISSN：1001-604X
  • 国内统一刊号：ISSN：31-1547/O6
  • 邮发代号:4-646
  • 获奖情况:
  • 中国期刊方阵“双高”期刊
  • 国内外数据库收录:
  • 美国化学文摘（网络版）,荷兰文摘与引文数据库,美国科学引文索引（扩展库）,日本日本科学技术振兴机构数据库,英国英国皇家化学学会文摘
  • 被引量:175