Facile Synthesis of Enantioenriched C<sup>γ</sup>-Tetrasubstituted α-Amino Acid Derivatives via an Asymmetric Nucleophilic Addition/Protonation Cascade
收藏NIAID Data Ecosystem2026-03-07 收录
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An asymmetric nucleophilic addition/protonation reaction of 3-substituted oxindoles and ethyl 2-phthalimidoacrylate has been described. This strategy can give direct access to Cγ-tetrasubstituted α-amino acid derivatives bearing 1,3-nonadjacent stereocenters with up to 98% yield, 94:6 dr, and >99% ee. Dual activation is proposed in the transition state, and the opposite enantiomers can be obtained simply by changing cinchonidine-derived catalyst to the cinchonine analogue.
创建时间：
2011-05-06
