Direct Copper‐Catalyzed α‐Arylation of Benzyl Phenyl Ketones with Aryl Iodides: Route towards Tamoxifen

G Danoun, A Tlili, F Monnier, M Taillefer - … Chemie International Edition, 2012 - infona.pl
G Danoun, A Tlili, F Monnier, M Taillefer
Angewandte Chemie International Edition, 2012infona.pl
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.
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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