Abstract: The research and development of effective anti-cancer drugs have been urgently needed. Molecular targeted drugs can be used to target tumor cells, which have good curative effect and little adverse reactions, and gradually become the development direction of anti-tumor drugs. As a molecular target drug Combretastatin A4 (CA₄) can inhibit tubulin polymerization and splitso that researchers pay more and more attention to the modification of CA4 structure and similar things. The development of this area becomes one of the direction of anti-tumor drugs research hot spot. This article presented an efficient synthesis method of 1-(3-methoxy-phenyl)-4-(4-Fluoro-2-methoxy-D₃-phenylaminemethyl-1H-1,2,3triazole with iodomethane-D₃ as the common substrate, which was mainly obtained through methylation, reduction, substitution,azidation and cyclization reaction. The yields of 1-(3-methoxy-phenyl)-4-(4-Fluoro-2-methoxy-D₃-phenylaminemethyl-1H-1,2,3triazole was 60.2% based on iodomethane-D₃ consumed. The chemical purity of this product was 99.0% and deuterium isotopic enrichment of this product was 99.0%. The compound could be used in the field of antitumor drug because of a broad range of anticancer activity of it.