Studies On Arylation Reaction Of N-heteroaromatics

N-heteroaromatics are a class of significant compounds applied widely in the synthesis of nature products,pharmaceuticals,agrochemicals and relative materials.Amongst them,arylated N-heteroaromatics(mainly arylated pyridines and arylated quinolines)have attracted attention due to their diverse bioactivity and application value.For the synthesis of N-heteroaromatics,the most prevalent strategy towards cross-coupling of N-heteroaromatic halides with different arylation reagents have been done by using transition metal catalysts.These reagents include aryl non-metallic and aryl metallic compounds(mainly phenylboronic acid),aryl sulfinates and arenes.Although these synthetic methods have promoted the considerable development of arylation of N-heteroaromatics,there were still some drawbacks.In order to solve these problems,we developed a novel method for synthsis of arylated N-heteroaromatics.The arylated products such as arylated pyridines and arylated quinolines have been synthesized by using hypervalent iodine compounds as arylation reagents under PdCl2/Cs2CO3 catalytic system.This process proceeded under simple and mild conditions without using ligands,and the operation was simple,the scopes of substrates were expanded with high yields as well.But the most important advantage was the excellent characteristics of hypervalent iodine compounds,which made the new method have much more superiority.