Abstract

Comprehensive SummaryChiral phosphoric acid catalyzed the regio‐ and enantioselective N—H functionalization of N‐alkylaniline with pyrazolones derived ketimines as electrophiles, providing a variety of chiral pyrazolones containing a tetrasubstituted stereocenter bearing a new N,N’‐acetal motif in excellent yields and high enantioselectivities. This strategy was featured by low catalyst loading, mild conditions, and high efficiency and selectivity.

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