Hypervalent Iodine Regants Mediated Selective Aromatic C-H Functionalization

The main content of this article is hypervalent iodine regants mediated armotic C-H functionalization,respectively,the amination or sulfonylation of 8-acylaminoquinolines and anilides.The reactions can be successfully applied for amination or sulfonylation,only mediated by hypervalent iodine regants,without any metal catalyst and other additives.The main contents are as follows:1.An oxidative C-H amination of 8-acylaminoquinolines and anilides with N-fluorobenzenesulfonimide(NFSI)has been developed,which mediated by hypervalent iodine regant PhI(OPiv)2 under mild reaction conditions without any metallic catalyst or oxidant.The protocol showed good air and moisture tolerance,functional groups compatibility,and gave the highly site-selective amination products in moderate to good yields,providing a novel and facile method for synthesis of arylamine compounds(Scheme 1).Scheme 12.On the basis of the previous research results,we begin to explore the range of application of hypervalent iodine regants mediated aromatic C-H functionalization.Then a highly site-selective oxidative C-H sulfonylation method for 8-acylaminoquinolines and anilides with sulfonyl chlorides has been developed,which provided the C5-sulfonylated quinolines and para-sulfonylated anilides respectively.Good functional group compatibility was showed in both amides and sulfonyl substrates.This method was only mediated by a hypervalent iodine reagent PhI(OPiv)2 under mild conditions without any metallic catalyst or extra additives,which would provide a novel and facile methodology for synthesis of sulfone compounds(Scheme 2).Scheme 2...