The first copper‐catalyzed highly chemo‐, regio‐, diastereo‐, and enantioselective Kinugasa/Michael domino reaction for the desymmetrization of prochiral cyclohexadienones is described. In the presence of a chiral copper catalyst, alkyne‐tethered cyclohexadienones couple with nitrones to generate the chiral spirocyclic lactams with excellent stereoselectivity (up to 97 % ee, >20:1 dr). The new method provides direct access to versatile highly functionalized spirocyclic β‐lactams possessing four contiguous stereocenters, including one quaternary and one tetra‐substituted stereocenter.

中文翻译：

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通过铜催化的衣笠/迈克尔多米诺反应不对称合成螺环β-内酰胺

描述了第一个铜催化的高度化学、区域、非对映和对映选择性 Kinugasa/Michael 多米诺反应，用于前手性环己二烯酮的去对称化。在手性铜催化剂存在下，炔烃环己二烯酮与硝酮偶联生成具有优异立体选择性（高达 97% ee，>20:1 dr）的手性螺环内酰胺。新方法提供了对具有四个连续立体中心（包括一个四取代立体中心和一个四取代立体中心）的多功能高度功能化的螺环 β-内酰胺的直接访问。