Abstract

Disclosed herein is an efficient organocatalytic formal N-H insertion reaction of arylamines with α-keto sulfoxonium ylides bearing two aryl groups, delivering a broad range of α-tertiary aminoketones with good to excellent yields and enantioselectivities (up to 90% yield and 94% ee). The utilities of this protocol were also demonstrated by facile preparation of enantioenriched 2-amino-1,2-diarylethanol bearing two different aryl groups, a type of important building block lacking efficient access.

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