Abstract: OBJECTIVE To improve the synthesis process of the anticancer drug Masitinib. METHODS Masitinib(1) was synthesized using 2-methyl-5-nitroaniline as the starting material, via addition, cyclization with self-made compound 2, reduction, and amidation with acyl chloride compound 3. RESULTS The total yield was 28.0% basing on the row material 2-methyl-5-nitroaniline and structures of the key intermediates and the target were confirmed by MS and 1H NMR. CONCLUSION Compared with the literature method, the improved process has the advantages of low-cost, convenient operation and broad prospects for commercial scale-up.