Highly Site- and Enantioselective N-H Functionalization of N-Monosubstituted Aniline Derivatives Affording Pyrazolones Bearing a Quaternary Stereocenter

摘要

Comprehensive Summary Chiral 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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