A new synthesis method of repaglinide industrialization was studied. 4-Carboxymethyl -2- ethoxy benzoic acid ester reacted with pivaloyl chloride to form active intermediate, thenby one pot method，2-oxethyl-4-{2-{[(1S) -3- methyl -1-[2- (1- piperidyl) phenyl] butyl]amino}-2- oxygen generation ethyl} ethyl benzoate was sythe-sized　from (S) -3- methyl -1-[2-(1-piperidyl) penyl] butylamine, the target compound was synthesized by the hydrolysis of repaglinide. The results ｓhowed　that　the new synthesis method of repaglinide had higher purity, higher yield　which　was up to 63%，a mild reaction　condition，convenient operation，friengly environment，and was suitable to large scale manufacturing.