College of Chemical Engineering, Zhejiang University of Technology, Chaowang Road 18, Hangzhou, 310014, China.
Angew Chem Int Ed Engl. 2017 Jun 19;56(26):7475-7478. doi: 10.1002/anie.201703833. Epub 2017 May 23.
Palladium-catalyzed enantioselective dearomative arylalkynylation of N-substituted indoles, through a Heck/Sonogashira sequence, was established using a new BINOL-based phosphoramidite as the chiral ligand. A wide range of 2,3-disubstituted indolines, bearing vicinal quaternary and tertiary stereocenters, were efficiently constructed in one step with excellent enantioselectivities (up to 97 % ee) and diastereoselectivities (>20:1).
钯催化的 N-取代吲哚的对映选择性去芳构化芳基炔基化反应，通过 Heck/Sonogashira 序列，使用新型 BINOL 衍生的手性磷酰胺作为手性配体得以建立。一系列 2,3-二取代的吲哚啉，具有相邻的季碳和三级立体中心，能够以优异的对映选择性（高达 97%ee）和非对映选择性（>20:1）一步高效构建。
