American Chemical Society
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Synthesis of 3-Substituted Isocoumarins via a Cascade Intramolecular Ullmann-Type Coupling–Rearrangement Process

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journal contribution
posted on 2012-07-06, 00:00 authored by Zhi-Yuan Ge, Xiang-Dong Fei, Ting Tang, Yong-Ming Zhu, Jing-Kang Shen
A simple and highly efficient strategy for the synthesis of 3-substituted isocoumarins through a copper­(I)-catalyzed reaction of 1-(2-halophenyl)-1,3-diones has been developed. The procedure is based on a cascade copper-catalyzed intramolecular Ullmann-type C-arylation and rearrangement process. This methodology is tolerant of a wide range of substrates and applicable to library synthesis.