Enantioselective three-component Ugi reaction catalyzed by chiral phosphoric acid

• 来源期刊: 中国科学:化学（英文版）
• 年，卷（期）: 2020,（1）
• 页码范围: 47-54
• 页数: 8页
• 语种: 英文

摘要

A catalytic enantioselective three-component Ugi reaction was developed.SPINOL-derived phosphoric acid with bulky 2,4,6-tricyclohexylphenyl groups at the 6,6'positions was found to be the best catalyst to afford αt-amino amide derivatives in good to excellent yields (62％ to 99％) and enantiocontrol (81％ to ＞99％ enantiomeric excess).This asymmetric reaction was applicable well to an array of aliphatic aldehydes.The gram-scale synthesis,modification ofdapsone,and enantioselective synthesis of(R)-Lacosamide underline the general utility of this methodology.Influence of dihedral angles and substituents of the chiral phosphoric acids on the enantioselectivity was also discussed in this article.