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Dipak D. Vachhani, Dr. Abhishek Sharma and Prof. Dr. Erik Van der Eycken Copper-Catalyzed Direct Secondary and Tertiary C[BOND]H Alkylation of Azoles through a Heteroarene–Amine–Aldehyde/Ketone Coupling Reaction Angewandte Chemie International Edition 52

Article first published online: 22 JAN 2013 | DOI: 10.1002/anie.201209312

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Coupling the strangers: A copper-catalyzed three-component heteroarene–amine–aldehyde/ketone coupling affords a novel approach to the hitherto difficult direct secondary/tertiary C[BOND]H alkylation of azoles. This simple method allows the facile installation of diversely substituted, branched and nitrogen-containing alkyl or alkaloid side chains on the azole moiety by using readily available starting materials (see scheme).

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