Abstract: Aiming at process optimization of synthesizes of 7′-Br-anhydrovinblastine from anhydrovinblastine; experiment factors and levels were firstly selected by single factor tests. According to the Box-Benhnken design principle，the method of response surface method with 3 factors and 3 levels was used. The factors influencing the technological parameters were determined by means of regression analysis. Response surfaces were finally graphed with the yield as the response value. The synthesis conditions were optimized as follows：reaction reagent was NBS，stoichiometric proportion between NBS and anhydrovinblastine was 1.07; the dosage of TFA was 22 mL/L; reaction temperature was －68 ℃ and duration was 90 min. The total yield of anhydrovinblastine to vinorelbine reached 70.56%.