Atropoenantioselective Arylation of 5‐Amino‐Isothiazoles with Methyl p ‐Quinone Carboxylate

Abstract Isothiazole units exist in many natural products and pharmaceutics. Up to now, construction of isothiazole‐containing axially chiral biaryls has not been reported yet. Herein we disclose a chiral phosphoric acid catalyzed atropoenantioselective arylation of 5‐amino‐isothiazoles with methyl p ‐quinone carboxylate. Various novel isothiazole‐containing axially chiral biaryls were achieved in moderate to good yields (up to 95%) with generally moderate to good enantioselectivities (up to 90% ee). In addition, the structure of one product was determined by an X‐ray crystal structural analysis and a plausible reaction mechanism was proposed.