Abstract

AbstractArylation of ketimines is the most straightforward strategy for constructing chiral α‐tertiary amines, important structural motifs found in natural products and biologically active compounds. This comprehensive review highlights the achievements in the transition metal‐catalyzed and organocatalyzed asymmetric arylations of ketimines from the seminal report published in 2010 till November 2023. The review is divided into three chapters: (1) Arylation of diaryl ketimines, (2) Arylation of aryl‐alkyl and aryl‐acyl ketimines, and (3) Arylation of acyl‐alkyl and dialkyl ketimines. Each chapter is further divided into transition metal‐catalyzed reactions (grouped by individual metals) and organocatalyzed reactions. The covered literature includes emphasis on the advantages of the reported methodology, its scope and limitations, and the description of the transition state (where applicable).

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