Biphenyl aldehyde-based ternary catalytic system catalyzed Tsuji–Trost allylation of N-unprotected amino acid esters

Abstract

A highly efficient biphenyl aldehyde-based ternary catalytic system is rationally designed and applied in the direct α-allylation reaction of N-unprotected amino acid esters and allyl alcohol acetates. The chemoselectivity of C-allylation and N-allylation is efficiently controlled and various racemic α,α-disubstituted amino acid esters are generated in good-to-high yields. The target products can be readily converted into structurally diverse α,α-disubstituted amino acids at a gram scale.