In this work, we have developed an efficient method for the intramolecular double hydroamination of aniline by employing -amino 1,6-diyne as a potential starting material. This protocol enables easy access to bioactive motif 3,4-dihydro-1-[1,4]oxazino[4,3-]indole through an intramolecular cascade bicyclization and concomitant isomerization pathway in one pot. This transformation has been effectively achieved by utilizing a stereoelectronically tuned, π-accepting NHC-supported copper(I) system.
View Article and Find Full Text PDFSelective functionalization of the indole-C3-C bond with aromatic/heteroaromatic 1,2-diketones has been uncovered for the first time. Cobalt catalyst was found to be an effective catalyst for this unusual transformation. This -C-C bond functionalization occurred in the presence of easily available weakly coordinating groups such as ketone and ester.
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