An Annulative Electrophilic Amination Approach to 3-Aminobenzoheteroles
The Journal of Organic Chemistry2011Vol. 77(1), pp. 617–625
Citations Over TimeTop 10% of 2011 papers
Abstract
A copper-catalyzed annulative amination approach to 3-aminobenzofurans and -indoles from o-alkynylphenols and -anilines has been developed. The Cu-based catalysis is based on an umpolung, electrophilic amination with O-benzoyl hydroxylamines and enables the mild and convergent synthesis of various 3-aminobenzoheteroles of biological and pharmaceutical interest. Some mechanistic investigations and an application of this protocol to construction of more complex tricyclic framework are also described.
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