Wang Kun, Yu Yan-Jiang, Wang Xiao-Qing, Bai Yu-Qing, Chen Mu-Wang, Zhou Yong-Gui
Zhang Dayu School of Chemistry, Dalian University of Technology, Dalian 116024, P. R. China.
State Key Laboratory of Catalysis, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, P. R. China.
J Org Chem. 2022 Aug 5;87(15):10398-10407. doi: 10.1021/acs.joc.2c00702. Epub 2022 Jul 22.
A palladium-catalyzed asymmetric hydrogenation of unprotected 3-substituted indoles was developed, providing a series of 3-substituted indolines in excellent yields with ≤94.4:5.6 er. The large sterically hindered bisphosphine ligand played a crucial role in the enantioselective control. In addition, the gram-scale hydrogenation experiment and product derivatizations were performed successfully.
开发了一种钯催化的未保护3-取代吲哚的不对称氢化反应，以优异的产率提供了一系列3-取代的二氢吲哚，对映体比例≤94.4:5.6。空间位阻较大的双膦配体在对映选择性控制中起关键作用。此外，还成功进行了克级氢化实验和产物衍生化。
