Synthesis of quinol-type heterobiaryls via an acid-catalyzed heteroannulation of alkynes and o-aminobenzaldehydes

Abstract

Herein, we report a practical strategy for the synthesis of structurally novel quinol-type heterobiaryls. A wide range of 1-(quinolin-2-yl)naphthalen-2-ols were afforded with good to excellent yields under mild reaction conditions. The synthetic utility of this protocol was further demonstrated by large-scale reaction. Furthermore, exploration on enantioselective synthesis of axially chiral C2-arylquinoline skeletons were also performed with good enantiopurity through a phase-transfer-catalyzed dynamic kinetic resolution.