Abstract

AbstractA method has been developed for the sulfonamidation of tetralones and 1,4‐naphthoquinones by using sulfonyl azides in the presence of a RuII/AgI catalytic system. In case of tetralones, C−H bond functionalization occurred exclusively at the ortho position, whereas 1,4‐addition was the main transformation for 1,4‐naphthoquinones. This method is highly regioselective and was successfully utilized for the synthesis of sivelestat, an inhibitor of human neutrophil elastase.

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