The invention relates to an
estrogen amino-acid ester compound with
antitumor activity as well as a synthetic method thereof, effectively solving the preparation problems of the
estrogen amino-acid ester compound with the
antitumor activity. The synthetic method comprises the following steps of: dissolving amino acids or
small molecule peptides to an
aqueous solution of
sodium hydroxide or a saturated solution of
sodium bicarbonate, dripping
carbobenzoxy chloride, making the solution react until the solution is not purple by developing with
ninhydrin or carrying out film detection; washing with aether, removing aether, adjusting the pH value of the water phase with
hydrochloric acid until milky white
solid occurs and extracting with
ethyl acetate; washing
mixed solution with
distilled water and saturated common
salt solution,
drying with
anhydrous magnesium sulfate, carrying out suction
filtration, concentrating and purifying; and then, mixing the
mixed solution with sterides
nucleus and dissolving the mixture to a reaction
solvent, adding a condensing agent and a catalyst, supplementing an additional condensing agent, carrying out film detection, filtering, concentrating and purifying, dissolving in a dissolving
solvent, adding
palladium carbon for
catalytic hydrogenation, detecting the film, filtering, concentrating and purifying. The
estrogen amino-acid ester compound withantitumor activity, provided by the invention, has favorable water
solubility and is superior to 2-methoxyestradiol in the tumor
cell resistance action.