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Dr. Grégory Danoun, Dr. Anis Tlili, Dr. Florian Monnier and Dr. Marc Taillefer Direct Copper-Catalyzed α-Arylation of Benzyl Phenyl Ketones with Aryl Iodides: Route towards Tamoxifen Angewandte Chemie International Edition 51

Article first published online: 9 NOV 2012 | DOI: 10.1002/anie.201206024

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No activation needed: The first efficient method for direct α-arylation of non-activated or non-protected family of enolizable ketones with simple aryl iodides employs a catalytic copper system. The method shows potential for the easy and step-economical synthesis of tamoxifen, the most commonly administrated drug for the management of breast cancer. R, R′, R′′ = electron-donating or electron-withdrawing groups.

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