Volume 3, Issue 2 (June, 2023) – 10 articles
Cover Picture: Quinidine-catalyzed regio- and enantioselective formal [4 + 2]-cycloadditions of 2-(4H-benzo[d][1,3]oxazin-4-yl)acrylates with N-tosyl-2-methylenebut-3-enoates and 2-methylene-3-oxoalkanoates have been developed for the first time. The reaction features the in situ formation of chiral nitrogen-containing dipolar intermediates, a ring-opening/Michael addition/annulation cascade reaction, and works well over a broad substrate scope to furnish the tetrahydroquinolines in high yields with high asymmetric induction under mild conditions.
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Cover Picture: The direct enantioselective construction of axially chiral 3-arylindole frameworks via nucleophilic addition of 2-substituted indoles to iminoquinones has been achieved with high efficiencies under mild chiral phosphoric acid (CPA) catalytic conditions. The utility of this method was demonstrated in successful scale-up syntheses without compromising the product yields and enantioselectivities. The oxidation of products yields axially chiral heteroaryl-p-quinone monoimine, which could be subjected to structural diversification via addition of nucleophiles.
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