The invention discloses a synthesis method of xanthinol nicotinate. The synthesis method comprises the following steps: synthesizing 2-hydroxy-3-(2-ethoxy-methylamino) chloropropane by epichlorohydrin and N-methylethanolamine; then reacting the 2-hydroxy-3-(2-ethoxy-methylamino) chloropropane with theophylline and niacin so as to synthesize crude xanthinol nicotinate; and finally, refining the crude xanthinol nicotinate so as to obtain the finished xanthinol nicotinate. The synthesis method is characterized in that solvents used when the 2-hydroxy-3-(2-ethoxy-methylamino) chloropropane is reacted with the theophylline and the niacin are absolute ethyl alcohol. Compared with a mixed solvent of toluene and isopropanol in the prior art, the absolute ethyl alcohol serving as a solvent in the invention has the advantages of cheap price and low toxicity, thereby lightening environmental pressure; and in addition, in the process, the purity and yield of the finished xanthinol nicotinate are improved through an improvement on activated carbon and a refining process. The process has the advantages that the route is clear, the operation is simple, the raw materials are saved and the cost isreduced, thus being beneficial to industrial mass production.