Chiral aldehyde catalysis enables direct asymmetric α-substitution reaction of N-unprotected amino acids with halohydrocarbons

作者：Haoran Shen, Chao-Xing Li, Xin Jiang, Yao Lin, Jianhua Liu, Fang Zhu, Zhu‐Lian Wu, Tian Cai, Wen Wei, Rongxing He, Qi‐Xiang Guo · 发表于：Chemical Science · 年份：2023 · DOI：10.1039/d3sc01294h · 被引用次数：20 · 研究领域：Asymmetric Synthesis and Catalysis、Asymmetric Hydrogenation and Catalysis、Synthesis and Catalytic Reactions

, the asymmetric α-arylation, α-allylation, and α-benzylation of amino acid esters with the corresponding halohydrocarbons proceed smoothly, producing α,α-disubstituted α-amino acids in moderate-to-high yields and good-to-excellent enantioselectivities. The asymmetric α-arylation reaction can be applied in the formal synthesis of the clinical candidate compound (+)-AG-041R. Based on the results given by control experiments, three reaction models are proposed to illustrate the stereoselective-control outcomes.