Direct and Selective 3-Amidation of Indoles Using Electrophilic N-[(Benzenesulfonyl)oxy]amides.
Selective C-H amidation of 1H-indoles at the C3 position is reported as a direct entry to biologically important 3-aminoindoles. This transformation is achieved using novel N-[(benzenesulfonyl)oxy]amides as electrophilic nitrogen agents in the presence of ZnCl2
. Interestingly, analogous reactions in the absence of ZnCl2
resulted in the formation of indole aminal products.
Ortiz, GX; Hemric, BN; Wang, Q
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