American Chemical Society
ol1c03688_si_001.pdf (6.04 MB)

Copper-Catalyzed Ullmann-Type Coupling and Decarboxylation Cascade of Arylhalides with Malonates to Access α‑Aryl Esters

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journal contribution
posted on 2021-12-21, 18:05 authored by Fei Cheng, Tao Chen, Yin-Qiu Huang, Jia-Wei Li, Chen Zhou, Xiao Xiao, Fen-Er Chen
We have developed a high-efficiency and practical Cu-catalyzed cross-coupling to directly construct versatile α-aryl-esters by utilizing readily available aryl bromides (or chlorides) and malonates. These gram-scale approaches occur with turnovers of up to 1560 and are smoothly conducted by the usage of a low catalyst loading, a new available ligand, and a green solvent. A variety of functional groups are tolerated, and the application occurs with α-aryl-esters to access nonsteroidal anti-inflammatory drugs (NSAIDs) on the gram scale.