Catalytic Enantioselective Aminopalladation–Heck Cascade
Yu‐Ping He, Jian Cao, Hua Wu, Qian Wang, Jieping Zhu
Abstract
Abstract Domino processes initiated by intramolecular nucleopalladation of alkynes have been developed into powerful synthetic tools for the synthesis of functionalized heterocycles. However, a catalytic enantioselective version of this class of reactions remains scarce. We report herein that reaction of 2‐alkynylanilines with prochiral cyclopentenes in the presence of a catalytic amount of Pd(OAc) 2 , a chiral bidentate pyrox ligand and O 2 as terminal oxidant affords the structurally diverse indole‐cyclopentene conjugates bearing two stereocenters in a highly diastereo‐ and enantio‐selective manner. One of the products is converted to a heavily functionalized tetracyclic indolinone derivative.