A catalytic enantioselective method for the synthesis of chiral 1H-isoindoles bearing quaternary stereogenic centers is reported. Powered by readily accessible phosphordiamidite ligands, the presented palladium(0)-catalyzed C-H function-alization uses trifluoroacetimidoyl chlorides as electrophilic components. It delivers previously inaccessible perfluoroalky-lated 1H-isoindoles in high yields and enantioselectivities. The subsequent diastereoselective addition of nucleophiles provides access to densely substituted and sterically hindered isoindolines.
Xile Hu, Chao Fan, Srikrishna Bera
Qian Wang, Jieping Zhu, Baochao Yang, Guang Li