He, Yu-PingWu, HuaWang, QianZhu, Jieping2020-01-292020-01-292020-01-29202010.1002/anie.201914049https://infoscience.epfl.ch/handle/20.500.14299/165011We report herein the first examples of a palladiumcatalyzed enantioselective Cacchi reaction for the synthesis of indoles bearing a chiral C2-aryl axis. In the presence of a catalytic amount of Pd(OAc)2 and (R,R)-QuinoxP* ligand, reaction of N-aryl(alkyl)sulfonyl-2-alkynylanilides with arylboronic acids under oxygen atmosphere afforded enantioenriched 2,3-disubstituted indoles in high yields and enantioselectivity. The indole ring is constructed de novo in this process and a complexation-induced chirality transfer is proposed to account for the observed enantioselectivity.asymmetric synthesisaxial chiralitycross-couplinghomogeneous catalysisindolestext::journal::journal article::research article