Key Laboratory of Regenerative Biology and Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, No. 190 Kaiyuan Avenue, Guangzhou Science Park, Guangzhou 510530, China.
J Am Chem Soc. 2012 Sep 5;134(35):14326-9. doi: 10.1021/ja306631z. Epub 2012 Aug 24.
The first highly enantioselective copper-catalyzed intramolecular Ullmann C-N coupling reaction has been developed. The asymmetric desymmetrization of 1,3-bis(2-iodoaryl)propan-2-amines catalyzed by CuI/(R)-BINOL-derived ligands led to the enantioselective formation of indolines in high yields and excellent enantiomeric excesses. This method was also applied to the formation of 1,2,3,4-tetrahydroquinolines in high yields and excellent enantioselectivity.
首次发展了高对映选择性的铜催化的内分子 Ullmann C-N 偶联反应。手性铜(I)/(R)-BINOL 衍生配体催化 1,3-双(2-碘芳基)丙-2-胺的不对称去对称化反应,以高产率和优异的对映选择性形成吲哚啉。该方法也适用于高产率和优异对映选择性的 1,2,3,4-四氢喹啉的形成。