镍/锌协同催化γ−酮酸的不对称氢化反应研究

Study on asymmetric hydrogenation of γ-keto acid catalyzed by Ni/Zn

  • 摘要: 手性γ−戊内酯是许多重要的天然产物和生物活性分子的结构单元之一. 文章报道一种廉价、高效制备手性γ−戊内酯的方法,以氢气为氢源,在镍−锌协同催化体系下,对市售芳基γ−酮酸进行不对称氢化反应,获得了一系列手性戊内酯衍生物. 该催化体系具有良好的底物适用性,收率高达99%,对映选择性高达98%,为获得有价值手性γ−戊内酯提供了一种高效、经济的方法,在有机合成和制药工业中具有重要的潜在应用前景.

     

    Abstract: Chiral γ-valerolactone is an important structural motif of many important natural products and bioactive molecules. This paper reports a cheap and efficient method to prepare chiral lactones. A series of chiral lactone derivatives were obtained by asymmetric hydrogenation of commercially available γ-aryl keto acids with hydrogen as hydrogen source with the Ni-Zn co-catalytic system. The catalytic system has shown good substrate applicability, affords corresponding chiral γ-valerolactones in up to 99% yield with up to 98% ee. The present methodology has provided an efficient and economical method for valuable chiral γ-valerolactones, and has important potential applications in organic synthesis and pharmaceutical industry.

     

/

返回文章
返回