Pd-catalyzed enantio-and diastereoselective synthesis of N-N atropisomeric indoles via N-alkylation reaction

Abstract

We disclose a method for the asymmetric synthesis of N-N axially chiral indole compounds by Pd-catalyzed N-alkylation reaction, featuring good substrate tolerance and yield with high enantio-and diastereoselectivity. Furthermore, the synthetic utility of the protocol was demonstrated by large-scale reaction and transformation of the product.