DOI: 10.1002/ajoc.70567 ISSN: 2193-5807

Efficient Arylation of Malonates/Cyanoacetates With Aryl Bromides via Ligand‐Enhanced Copper Catalysis

Shigang Wu, Hepu Cheng, Gang Zou

ABSTRACT

An oxalamide/copper catalyst system has been developed for efficient arylation of malonates/cyanoacetates with aryl bromides for highly selective access to aryl malonates and cyanoacetates. Use of excess (2.5 equiv.) malonate/cyanoacetate has been found to not only accelerate the arylation but also suppress the decarboxylation side reaction. Scope and limitations of the protocol have been demonstrated by >47 examples, showing good compatibility with common functional groups but large steric effects from both aryl bromide and malonate/cyanoacetate counterparts. A series of aryl malonates/cyanoacetates could be obtained in good to excellent yields using this practical protocol.

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