Abstract

A highly regioselective 5-exo-dig cyclization of aromatic N-propargyloxycarbonyl guanidines was developed via an Ag(I)-catalyzed intramolecular hydroamination reaction. This method features a fast reaction rate and mild reaction conditions. Furthermore, it was extended to access halogenated analogues via a one-pot Ag(I)-catalyzed bromocyclization reaction or an I2-mediated iodocyclization reaction with high E/Z selectivity.

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