Enantioselective Alkynylation of 2‐Aryl‐3H‐indol‐3‐ones via Cooperative Catalysis of Copper/Chiral Phosphoric Acid

Abstract

A facile enantioselective alkynylation of cyclic ketimines attached to a neutral functional group utilizing the dual Cu(I)‐CPA catalysis is described. The strategy of the alkynylation of 2‐aryl‐3H‐indol‐3‐one directly to chiral propargylic amines containing indolin‐3‐one moiety in good yields and enantioselectivities. Moreover, gram‐scale synthesis of chiral propargylamines based C2‐quaternary indolin‐3‐ones was performed. The synthetic applications were confirmed by transformations of the products with no decrease in the yield and enantioselectivity.