An efficient and facile process was developed for the remote C-H bond amidation of 8-aminoquinoline scaffolds on the C5 position which is geometric. The method only made use of PhI(OAc)2 as a mediator and showed good tolerance toward numerous dibenzenesulfonimides and amides, giving the corresponding products in moderate to excellent yield.

Direct regioselective halogenation of 8-amidoquinolines on the C5 position in the presence of NFSI and CuX under mild conditions.

A novel and efficient method for direct tosyloxylation at C5 position of 8‐aminoquinolines has been accomplished by nonmetal‐catalyzed C–H functionalization at mild conditions. It is shown, for the first time, that the radical RSO3· could be generated by the reaction of phenyliodine bistrifluoroacetate with substituted 1,2‐disulfonyl hydrazides. This reaction reveals excellent reactivity, good functional group tolerance, and moderate to good yield.

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