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Palladium(II)-Catalyzed Intramolecular Diamination of Alkynes under Aerobic Oxidative Conditions: Catalytic Turnover of an Iodide Ion


  • We thank the EPFL (Switzerland), the Swiss National Science Foundation (SNF), and the Swiss National Centres of Competence in Research (NCCR) for financial support.


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“I” did it: A sequential intramolecular amination/N-demethylation/amidation of internal acetylenes in the presence of a catalytic amount of Pd(OAc)2 and nBu4NI afforded indolo[3,2-c]isoquinolinones under mild aerobic conditions (see scheme, DMSO=dimethyl sulfoxide). The iodide ion was regenerated by reaction of in situ generated MeI with HOAc present in the reaction mixture.