Direct and Selective 3-Amidation of Indoles Using Electrophilic N-[(Benzenesulfonyl)oxy]amides.

ABSTRACT: 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.

SUBMITTER: Ortiz GX 

PROVIDER: S-EPMC5685508 | biostudies-literature | 2017 Mar

REPOSITORIES: biostudies-literature