Access to Sultams by Rhodium(III)-Catalyzed Directed C-H Activation

摘要

The aryl sulfonamide moiety is a very important and ubiquitous functional group which is closely linked to pharmaceutical activity, and plays a significant role as a structural design element in medicinal chemistry. Both primary sulfonamides and sulfonyl ureas are common motifs is drugs as exemplified by celecoxib, brinzolamide, sultiame, and glibenclamide (Figure 1). Acylated sulfonamides, which are subject to facile deacylation, can be used as prodrugs. Besides aryl sulfonamides, their cyclic analogues, benzosul-tams, play an important role given their broad biological activities. Piroxicam and brinzolamide demonstrate the utility of annulated sultams.