Direct arylation of cyclopentanones has been a long-standing challenge because of competitive self-aldol condensation and multiple arylations. Reported herein is a direct mono-α-C-H arylation of cyclopentanones with aryl bromides which is enabled by palladium/amine cooperative catalysis. This method is scalable and chemoselective with broad functional-group tolerance. Application to controlled sequential arylation of cyclopentanones has been also demonstrated.
Direct arylation of cyclopentanones has been a long‐standing challenge because of competitive self‐aldol condensation and multiple arylations. Reported herein is a direct mono‐α‐C−H arylation of cyclopentanones with aryl bromides which is enabled by palladium/amine cooperative catalysis. This method is scalable and chemoselective with broad functional‐group tolerance. Application to controlled sequential arylation of cyclopentanones has been also demonstrated.
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