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Direct Copper‐Catalyzed α‐Arylation of Benzyl Phenyl Ketones with Aryl Iodides: Route towards Tamoxifen
Author(s) -
Danoun Grégory,
Tlili Anis,
Monnier Florian,
Taillefer Marc
Publication year - 2012
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201206024
Subject(s) - aryl , tamoxifen , catalysis , combinatorial chemistry , copper , chemistry , breast cancer , organic chemistry , cancer , medicine , alkyl
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.