Bifunctional Organocatalysts for the Enantioselective Synthesis of Axially Chiral Isoquinoline <i>N</i>‑Oxides

Bifunctional catalysts bearing amino and urea functional groups have been applied for a novel, highly enantioselective synthesis of axially chiral isoquinoline N-oxides, which are promising chiral ligands or organocatalysts in organic synthesis. This is the first example of highly enantioselective synthesis of axially chiral biaryls by bifunctional organocatalysts. Good-to-excellent enantioselectivities were obtained with a range of substrates.兼具氨基与脲基官能团的双功能催化剂，已被用于合成一类新型、高对映选择性的轴手性异喹啉N-氧化物。这类轴手性异喹啉N-氧化物在有机合成中是极具应用潜力的手性配体或有机催化剂。本研究为首例通过双功能有机催化剂实现轴手性联芳类化合物高对映选择性合成的案例。针对一系列底物，该方法均可获得良好至优异的对映选择性。