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

Danoun Grégory | Zendy; Tlili Anis | Zendy; Monnier Florian | Zendy; Taillefer Marc | Zendy

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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.

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