Dearomatization [4+2] cycloaddition for constructing bridged polycyclic lactams
Qile Wu1, Jingyi Chen1, Haoxian Wu1
1School of Environmental and Chemical Engineering, Wuyi University, Jiangmen 529020, China. chenxiuwen2010@126.com.
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This article presents a metal-free catalytic system for the [4+2] cycloaddition of isoquinoline and maleimide derivatives, enabling the one-step construction of structurally complex bridged polycyclic lactams. This three-component tandem cyclization reaction generates C-N, CO, and C-C bonds, achieving functionalization at the C1, N2, C3, and C4 positions of 3-halogenated isoquinolines. This dearomatization strategy exhibits exceptional chemoselectivity and regioselectivity, operates without transition metals, and offers a high atom and step economy.
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