A nickel‐catalyzed three‐component carboamination tandem cyclization strategy has been developed for the synthesis of 2,3‐disubstituted quinolines from propargyl alcohols, organoboronic acids, and anthranils. A novel α,β‐unsaturated imine intermediate plays a pivotal role in this system, undergoing base‐mediated annulation to assemble the quinoline core structure. This protocol exhibits good functional group tolerance and can be applied to the synthesis of 2,3‐unsymmetrically disubstituted quinolines and 2‐vinyl quinolines.
Xing et al. (Fri,) studied this question.