The invention discloses a preparation method of a
dehydroepiandrosterone-3beta-ester-5, 6-dimethyl
benzimidazole bromine salt derivative, which comprises the following steps: mixing
dehydroepiandrosterone,
chloroacetyl chloride, an
organic solvent and an activating-acid-binding agent, and carrying out
acetylation reaction to generate
dehydroepiandrosterone-3beta-ester; mixing the dehydroepiandrosterone-3beta-ester, 5, 6-dimethyl
benzimidazole and methylbenzene, and then carrying out a
substitution reaction, so as to obtain the dehydroepiandrosterone-3beta-ester-5, 6-dimethyl
benzimidazole, namely the dehydroepiandrosterone-3beta-ester-5, 6-dimethyl benzimidazole. And mixing the dehydroepiandrosterone-3beta-ester-5, 6-dimethyl benzimidazole,
alkyl bromide and
toluene, and then carrying out a salt forming reaction, so as to obtain the dehydroepiandrosterone-3beta-ester-5, 6-dimethyl benzimidazole
bromine salt derivative, namely the dehydroepiandrosterone-3beta-ester-5, 6-dimethyl benzimidazole
bromine salt derivative. The dehydroepiandrosterone-3beta-ester-5, 6-dimethyl benzimidazole bromine salt derivative obtained by the method has remarkable in-vitro
tumor growth inhibition activity on
human cancer cells, and the in-vitro
tumor growth inhibition activity of the dehydroepiandrosterone-3beta-ester-5, 6-dimethyl benzimidazole bromine salt derivative is superior to that of an anti-
cancer drug-cis-
platinum (DDP); meanwhile, the preparation method provided by the invention is simple and convenient to operate and easy to implement.