Hefei National Laboratory for Physical Sciences at the Microscale and Department of Chemistry, University of Science and Technology of China, 96 Jinzhai Road, Hefei, Anhui 230026, China.
Chem Commun (Camb). 2020 Oct 1;56(78):11605-11608. doi: 10.1039/d0cc05219a.
Enantioselective synthesis of tetrahydroisoquinolines bearing an all-carbon quaternary stereogenic center, was achieved via asymmetric C-H activation with high enantioselectivities (up to 93% ee). Fair substrate tolerance was indicated throughout the scope investigation and no evident loss of enantioselectivity was exhibited in late-stage derivatization. This study provides incentives for the construction of diverse chiral isoquinoline derivatives, which are prevalent among pharmaceuticals, natural products, etc.
通过不对称 C-H 活化反应,实现了具有全碳季立体中心的四氢异喹啉的对映选择性合成,具有很高的对映选择性(高达 93%ee)。在整个范围研究中,表现出良好的底物耐受性,并且在后期衍生化中没有明显的对映选择性损失。这项研究为构建各种手性异喹啉衍生物提供了动力,这些衍生物在药物、天然产物等中很常见。