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镍螯合物(II) Suzuki 偶联反应诱导的α-取代β-氨基酸的合成

吕丽, 王江, 丁晓, 林岱宗, 赵临襄, 蒋华良, 柳红*   

  1. 1. 中国科学院 上海药物研究所 新药研究国家重点实验室, 上海 201203
    2. 沈阳药科大学 制药工程学院, 辽宁 沈阳 110016
  • 收稿日期:2012-05-18 修回日期:2012-08-20 出版日期:2012-10-25 发布日期:2012-10-25
  • 通讯作者: 柳红*

Synthesis of α-substituted β-amino acids via the Ni(II) complex through the Suzuki coupling reaction

Li Lv, Jiang Wang, Xiao Ding1, Daizong Lin1, Linxiang Zhao2, Hualiang Jiang, Hong Liu*   

  1. 1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China
    2. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
  • Received:2012-05-18 Revised:2012-08-20 Online:2012-10-25 Published:2012-10-25
  • Contact: Hong Liu*

摘要:

镍螯合物2与多种取代的硼酸/硼酸酯3通过Suzuki 偶联反应, 制备具有多种取代的镍螯合物4, 通过氢化、水解两步反应合成α-取代β-氨基酸及其衍生物。该合成方法操作简单, 条件温和, 适用于α-取代-β-氨基酸及其衍生物的大规模制备。

关键词: 镍螯合物, Suzuki 偶联反应, α-取代β-氨基酸

Abstract:

A convenient and efficient method for the preparation of α-substituted β-amino acids has been developed by reacting compound 2 with various boric acid/borate 3 through Suzuki coupling reaction, which gave multiple structure types of substituted Ni(II) complexes 4 in high yields. Hydrogenation and hydrolysis of complexes 4 led to the corresponding α-substituted β-amino acids.

Key words: Ni(II) complex, Suzuki coupling reaction, α-Substituted β-amino acids

中图分类号: 

Supporting:

Foundation items: National Basic Research Program of China (Grants No. 2009CB940903 and 2009CB918502), the National Natural Science Foundation of China (Grant No. 20721003 and 81025017), and National S&T Major Projects (Grant No. 2012ZX09103-101-072).
*Corresponding author. Tel.: 86-21-5080742