The reaction of anhydrovinblastine (I) with m-chloroperbenzoic acid in dichloromethane gives anhydrovinblastine-N6-oxide (II), which by reaction with trifluoroacetic anhydride is converted to the bistrifluoroacetate (III). Compound (III) by treatment with THF-water undergoes isomerization to the open bistrifluoroacetate (IV), and cyclization to the desired product.