Abstract
A simple C-H/N-H bond functionalization of N-aryl amidines with cyclic 2-diazo-1,3-diketones for the synthesis of 1-aminoisoquinolines has been accomplished by employing [Cp*RhCl2]2/CsOPiv as the catalyst system. This methodology proceeds by a cascade C-H activation/intramolecular cyclization under mild reaction conditions, features a broad substrate scope, and involves the formation of two new σ bonds (C-C and C-N) in a single operation for the construction of novel 1-aminoisoquinoline skeletons in good to excellent yields.
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