A highly enantioselective aza-Friedel–Crafts arylation of biphenyl-bridged seven-membered cyclic N-sulfonylimines with indolizines was developed, affording a wide range of chiral indolizine modified biphenyl-bridged ε-sultams in excellent yields (up to 99% yield) and enantioselectivities (up to 99% ee) by utilizing chiral phosphoric acid organocatalysis. Furthermore, scale-up reactions and diversified synthetic transformations of the desired ε-sultams without the loss of stereochemical purity substantiated their potential utility values.

中文翻译：

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手性磷酸催化通过环状 N-磺酰亚胺与中氮茚的 Friedel-Crafts 反应对映选择性合成联苯桥联 ε-磺内酰胺


开发了联苯桥七元环状 N-磺酰亚胺与中氮茚的高度对映选择性氮杂-弗里德尔-克来福特芳基化反应，以优异的产率（高达 99% 产率）提供了多种手性中氮茚修饰的联苯桥 ε-磺内酰胺利用手性磷酸有机催化实现对映选择性（高达 99% ee）。此外，在不损失立体化学纯度的情况下，所需ε-磺内酰胺的放大反应和多样化合成转化证实了其潜在的实用价值。