Provided are an imidazo[1,2-a]pyridine-3-carboxylate derivative and a preparation method thereof, and more particularly, a method of effectively preparing an imidazo[1,2-a]pyridine-3-carboxylate derivative by performing an aza-[3+2] cycloaddition reaction of a pyridine derivative with an α-diazo oxime ether derivative in the presence of a copper (II) catalyst, and an imidazo[1,2-a]pyridine-3-carboxylate derivative prepared thereby.