Abstract

AbstractHerein, we report synergistic copper/amine‐catalyzed reactions for directly α‐benzylating carbonyl compounds with arylacetic acids. These reactions represent the first examples of decarboxylative oxidative synergistic transition‐metal/enamine catalysis for α‐functionalizing carbonyl compounds. The process features starting‐material availability, good functional group tolerance, mild reaction conditions, and good‐to‐excellent yields. Dibenzylated products were formed in moderate yields under slightly altered reaction conditions, and some products were transformed into 1,2,3,4‐tetrahydrocyclopenta[b]indole derivatives by acid‐catalyzed intermolecular cyclization reactions with indoles. Moreover, biological studies revealed that some products have anticancer properties and may be useful in drug‐discovery studies.magnified image

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