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Disclosed herein is a novel Rh/Ag co-catalyzed SNH directed C–H activation and C–H/N–H bond functionalization protocol of free NH-sulfoximines with hypervalent iodonium ylides. With the aid of AgOTf, these C–H functionalization/cyclization sequences could be achieved at room temperature conditions. The reaction employed EtOH as a “green” solvent and low catalyst loading was required under an oxygen/water-insensitive condition. Under this mild protocol, a wide range of polyheterocyclic sulfoximines bearing fused saturated carbo(hetero)cycles are readily prepared, even toward a complex pharmaceutical Folliculin analog.