Max-Planck-Institut für Kohlenforschung, Kaiser-Wilhelm-Platz 1, 45470, Mülheim an der Ruhr, Germany.
Angew Chem Int Ed Engl. 2016 Feb 5;55(6):2248-51. doi: 10.1002/anie.201507630. Epub 2016 Jan 14.
Aryl-substituted amino alcohols are privileged scaffolds in medicinal chemistry and natural products. Herein, we report that an exceptionally simple and inexpensive Fe(II) complex efficiently catalyzes the direct transformation of simple alkenes into unprotected amino alcohols in good yield and perfect regioselectivity. This new catalytic method was applied in the expedient synthesis of bioactive molecules and could be extended to aminoetherification.
芳基取代的氨基醇是药物化学和天然产物中的重要结构骨架。本文报道了一种非常简单且廉价的 Fe(II)配合物可高效催化简单烯烃直接转化为未保护的氨基醇,具有很好的收率和区域选择性。该新催化方法可用于生物活性分子的快速合成,并可扩展至氨基醚化反应。