The regioselective annulation of alkylidenecyclopropanes by Rh(iii)-catalyzed C-H/C-C activation to access spirocyclic benzosultams.


State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, P. R. China. [Email]


Functionalized benzosultams are an essential class of structural motif found in various biologically active molecules. The synthesis of spirocyclic benzosultams from N-sulfonyl ketimine and alkylidenecyclopropanes (ACPs) under the catalysis of Rh(iii) has been developed. This transformation enables the formation of two C-C bonds and a double bond with high E-selectivity through C-H and C-C bond activation. This reaction proceeded smoothly with excellent regioselectivity, high efficiency, and tolerance for various functional groups.

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