3-Indolylglycine and its derivates are versatile motifs in natural products,asymmetric chemical investigations,medicinal and peptide/peptidomimetic chemistry and drug discovery.Despite the fact that the approaches of enzymatic resolution and asymmetric synthesis have been reported,it is still significant to develop a highly enantioenriched synthetic method of 3-indolylglycines.The oxidative heterocoupling reaction of NH-containing heterocycles and carbonyl compounds exhibits high levels of chemoselectivity(functional group tolerability),regioselectivity(coupling occurs exclusively at C-3 of indole) and practicality(amenable to scaleup).