Palladium-catalyzed difunctionalization of alkynes via C-N and S-N cleavages: A versatile approach to highly functional indoles

Article abstract of DOI:10.1021/ol5024745

Palladium-catalyzed intramolecular addition of C-N and S-N bond to alkynes with the migration of functional groups has been achieved. A wide range of functional groups including acyl, pyruvoyl, amide, and sulfonyl groups can migrate smoothly and be conveniently introduced at the C-3 postion of indoles in our catalytic system. The operational simplicity and broad substrate scope demonstrate the great potential of this method for the synthesis of highly functional indoles.