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Copper‐Catalyzed Direct Secondary and Tertiary CH Alkylation of Azoles through a Heteroarene–Amine–Aldehyde/Ketone Coupling Reaction
Author(s) -
Vachhani Dipak D.,
Sharma Abhishek,
Van der Eycken Erik
Publication year - 2013
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.201209312
Subject(s) - aldehyde , ketone , moiety , alkylation , chemistry , amine gas treating , azole , database , combinatorial chemistry , catalysis , organic chemistry , computer science , antifungal , medicine , dermatology
Coupling the strangers : A copper‐catalyzed three‐component heteroarene–amine–aldehyde/ketone coupling affords a novel approach to the hitherto difficult direct secondary/tertiary CH 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).