有机化学 ›› 2008, Vol. 28 ›› Issue (06): 937-945.    下一篇

综述与进展

立体选择性还原的硼试剂及其在手性药物合成中的应用

蔡正艳*,周伟澄   

  1. (上海医药工业研究院 创新药物与制药工艺国家重点实验室 上海 200437)
  • 收稿日期:2007-06-06 修回日期:2007-09-19 发布日期:2008-06-26
  • 通讯作者: 蔡正艳

Application of Some Boron Reagents to Stereoselective Reduction in Synthesis of Chiral Drugs

CAI Zheng-Yan*, ZHOU Wei-Cheng   

  1. (State Key Laboratory of New Drug & Pharmaceutical Process, Shanghai Institute of Pharmaceutical Indus-try,
    Shanghai 200437)
  • Received:2007-06-06 Revised:2007-09-19 Published:2008-06-26
  • Contact: CAI Zheng-Yan

硼试剂在药物化学合成中广泛应用. 综述了可参与立体选择性还原反应的手性硼试剂、烷基硼试剂和硼氢化钠衍生物在手性药物合成中的应用, 并讨论这些试剂用于工业化生产的潜力.

关键词: 硼试剂, 立体选择性, 手性药物

Boron reagents have been applied widely to the synthesis of chiral drugs. This paper reviews the recent applications of chiral boron reagents, alkyl boranes and the derivatives of sodium borohydride to chiral drug synthesis via the stereoselective reduction of ketones to chiral alcohols. The potential of these boron reagents for industrialization is discussed.

Key words: stereoselectivity, chiral drug, boron reagent