Direct copper-catalyzed α-arylation of benzyl phenyl ketones with aryl iodides: Route towards tamoxifen

Abstract

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. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.