Development of catalytic asymmetric addition reactions via direct nucleophilic activation of unactivated C-H bonds

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Throughout this study, we developed direct catalytic asymmetric addition reactions via nucleophilic C-H bond activation, and we succeeded in obtaining alpha-amino acid derivatives containing chiral tetrasubstituted carbon stereocenters under proton-transfer conditions. The reactions proceed at or below room temperature, and various acid- and base-sensitive functionalities are tolerant under the reaction conditions.We also performed detailed mechanistic analysis of the reaction and isolated catalytically active species. This active species enabled shortening reaction time and performing reactions with other less-reactive substrates to provide alpha-amino acid derivatives containing chiral tetrasubstituted carbon stereocenters.